JP2015508086A5 - - Google Patents
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- JP2015508086A5 JP2015508086A5 JP2014558028A JP2014558028A JP2015508086A5 JP 2015508086 A5 JP2015508086 A5 JP 2015508086A5 JP 2014558028 A JP2014558028 A JP 2014558028A JP 2014558028 A JP2014558028 A JP 2014558028A JP 2015508086 A5 JP2015508086 A5 JP 2015508086A5
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- JP
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- Prior art keywords
- disease
- cancer
- prevention
- treatment
- medicament
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- 239000004480 active ingredient Substances 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 210000003128 Head Anatomy 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- 208000006673 Asthma Diseases 0.000 claims 1
- 210000004369 Blood Anatomy 0.000 claims 1
- 210000000988 Bone and Bones Anatomy 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000008787 Cardiovascular Disease Diseases 0.000 claims 1
- 206010039499 Cartilage sarcomas Diseases 0.000 claims 1
- 208000005145 Cerebral Amyloid Angiopathy Diseases 0.000 claims 1
- 210000003679 Cervix Uteri Anatomy 0.000 claims 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 1
- 201000010450 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- 201000010374 Down syndrome Diseases 0.000 claims 1
- 210000000981 Epithelium Anatomy 0.000 claims 1
- 210000003238 Esophagus Anatomy 0.000 claims 1
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- 208000007465 Giant Cell Arteritis Diseases 0.000 claims 1
- 208000005017 Glioblastoma Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 241000711549 Hepacivirus C Species 0.000 claims 1
- 208000009889 Herpes Simplex Diseases 0.000 claims 1
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- 201000001971 Huntington's disease Diseases 0.000 claims 1
- 210000000987 Immune System Anatomy 0.000 claims 1
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010022114 Injury Diseases 0.000 claims 1
- 210000000936 Intestines Anatomy 0.000 claims 1
- 210000003734 Kidney Anatomy 0.000 claims 1
- 241000222722 Leishmania <genus> Species 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 210000004185 Liver Anatomy 0.000 claims 1
- 210000004072 Lung Anatomy 0.000 claims 1
- 210000004324 Lymphatic System Anatomy 0.000 claims 1
- 206010025650 Malignant melanoma Diseases 0.000 claims 1
- 210000001616 Monocytes Anatomy 0.000 claims 1
- 241000186367 Mycobacterium avium Species 0.000 claims 1
- 241000186362 Mycobacterium leprae Species 0.000 claims 1
- 210000003739 Neck Anatomy 0.000 claims 1
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 1
- 206010061536 Parkinson's disease Diseases 0.000 claims 1
- 210000003800 Pharynx Anatomy 0.000 claims 1
- 210000002307 Prostate Anatomy 0.000 claims 1
- 206010072736 Rheumatic disease Diseases 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 241000700584 Simplexvirus Species 0.000 claims 1
- 206010040767 Sjogren's syndrome Diseases 0.000 claims 1
- 208000000587 Small Cell Lung Carcinoma Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 210000002784 Stomach Anatomy 0.000 claims 1
- 206010043207 Temporal arteritis Diseases 0.000 claims 1
- 210000001685 Thyroid Gland Anatomy 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 210000003932 Urinary Bladder Anatomy 0.000 claims 1
- 230000000172 allergic Effects 0.000 claims 1
- 201000003076 angiosarcoma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 230000002490 cerebral Effects 0.000 claims 1
- 201000003883 cystic fibrosis Diseases 0.000 claims 1
- 201000009910 diseases by infectious agent Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000011240 frontotemporal dementia Diseases 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 230000002757 inflammatory Effects 0.000 claims 1
- 230000000302 ischemic Effects 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 201000004792 malaria Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000002503 metabolic Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000004404 neurofibroma Diseases 0.000 claims 1
- 230000002314 neuroinflammatory Effects 0.000 claims 1
- 210000000056 organs Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 244000045947 parasites Species 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 201000004681 psoriasis Diseases 0.000 claims 1
- 230000000552 rheumatic Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 230000001732 thrombotic Effects 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 210000001331 Nose Anatomy 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 210000003928 Nasal Cavity Anatomy 0.000 description 1
- 229940100662 Nasal Drops Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
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- 230000000717 retained Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Description
担体物質が固体である、経鼻投与に適合された医薬製剤には、例えば２０〜５００ミクロンの範囲の粒径を有し、鼻から吸い込んで摂取される方法で、すなわち鼻の近傍に保持され、粉末を含有する容器から鼻腔を経由した急速な吸入により投与される粗粉末を含む。担体物質として液体を伴う鼻腔用スプレーまたは点鼻剤に好適な製剤には、水または油中の活性成分溶液が包含される。
Claims (9)
- 請求項１または２に記載の少なくとも１種の化合物、および／または、その薬学的に許容し得る塩、溶媒和物、互変異性体もしくは立体異性体、またはあらゆる比率のそれらの混合物、および、任意に、薬学的に許容し得る担体、賦形剤または溶媒を含む医薬。
- 炎症症状、免疫症状、自己免疫症状、アレルギー症状、リウマチ症状、血栓症状、がん、感染、神経変性疾患、神経炎症疾患、循環器疾患、および代謝症状の処置ならびに／または防止のための、請求項４に記載の医薬。
- 処置されるがんが、固形腫瘍または血液および免疫系の腫瘍である、がんの処置および／または防止のための請求項５に記載の医薬。
- 固形腫瘍が、上皮、膀胱、胃、腎臓、頭頸部、食道、子宮頸部、甲状腺、腸、肝臓、脳、前立腺、尿生殖路、リンパ系、喉頭、軟骨肉腫およびユーイング肉腫を含む骨、胚組織腫瘍を含む生殖細胞、ならびに／または肺の腫瘍の群に由来し、単球白血病、肺腺がん、小細胞肺がん、膵臓がん、神経膠芽腫、神経線維腫、血管肉腫、乳がんおよび／または悪性黒色腫の群に由来する請求項６に記載の医薬。
- リウマチ性関節炎、全身性紅斑性、喘息、多発性硬化症、骨関節炎、虚血損傷、巨細胞動脈炎、炎症性腸疾患、糖尿病、嚢胞性繊維症、乾癬、シェーグレン症候群および臓器移植拒絶の群から選択される疾患の処置および／または防止のための、請求項５に記載の医薬。
- アルツハイマー疾患、ダウン症候群、遺伝性アミロイド性脳出血−オランダ型、脳アミロイド血管症、クロイツフェルトヤコブ病、前頭側頭型認知症、ハンチントン病、パーキンソン病の群から選択される疾患の処置および／または防止のための請求項５に記載の医薬。
- リーシュマニア、M. leprae、M. tuberculosisおよび／またはM. aviumを含むマイコバクテリア、マラリア原虫、ヒト免疫不全ウイルス、エプスタインバーウイルス、単純ヘルペスウイルス、Ｃ型肝炎ウイルス
の群から選択される疾患の処置および／または防止のための請求項５に記載の医薬。 - 少なくともさらなる１種の医薬活性成分を含む、請求項４〜１０のいずれか一項に記載の医薬。
- （ａ）請求項１または２に記載の化合物および／またはその薬学的に許容し得る塩、溶媒和物、塩もしくは立体異性体、またはあらゆる比率でのそれらの混合物の有効量
および
（ｂ）さらなる医薬活性成分の有効量
の別々の包装からなるセット（キット）。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12001153 | 2012-02-21 | ||
| EP12001153.1 | 2012-02-21 | ||
| PCT/EP2013/000189 WO2013124026A1 (en) | 2012-02-21 | 2013-01-22 | 8 - substituted 2 -amino - [1,2,4] triazolo [1, 5 -a] pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017173002A Division JP2018039805A (ja) | 2012-02-21 | 2017-09-08 | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015508086A JP2015508086A (ja) | 2015-03-16 |
| JP2015508086A5 true JP2015508086A5 (ja) | 2016-03-17 |
| JP6479476B2 JP6479476B2 (ja) | 2019-03-06 |
Family
ID=47598786
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014558028A Active JP6479476B2 (ja) | 2012-02-21 | 2013-01-22 | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
| JP2017173002A Withdrawn JP2018039805A (ja) | 2012-02-21 | 2017-09-08 | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017173002A Withdrawn JP2018039805A (ja) | 2012-02-21 | 2017-09-08 | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9120804B2 (ja) |
| EP (1) | EP2817310B1 (ja) |
| JP (2) | JP6479476B2 (ja) |
| CN (1) | CN104114557B (ja) |
| AR (1) | AR090104A1 (ja) |
| AU (1) | AU2013224421B2 (ja) |
| CA (1) | CA2863723C (ja) |
| ES (1) | ES2674451T3 (ja) |
| IL (1) | IL233982A (ja) |
| TW (1) | TW201339165A (ja) |
| WO (1) | WO2013124026A1 (ja) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2674451T3 (es) * | 2012-02-21 | 2018-06-29 | Merck Patent Gmbh | 2-amino-[1,2,4]triazolo[1,5-a] pirazinas 8-sustituidos como inhibidores de la SYK tirosina quinasa e inhibidores de la serina quinasa GCN2 |
| NO2699580T3 (ja) | 2014-01-24 | 2018-02-24 | ||
| MX2017004506A (es) * | 2014-10-06 | 2017-08-15 | A Anton Mark | Implantes de seno recubiertos con politetrafluoroetileno expandido para minimizar la reacción capsular e infecciones, al mismo tiempo que reducen la palpabilidad. |
| WO2017189386A1 (en) * | 2016-04-29 | 2017-11-02 | Iomet Pharma Ltd. | Novel substituted imidazopyridine compounds as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan-2,3-dioxygenase |
| CN110382508B (zh) | 2016-12-22 | 2022-08-02 | 卡里塞拉生物科学股份公司 | 用于抑制精氨酸酶活性的组合物和方法 |
| GB201709456D0 (en) | 2017-06-14 | 2017-07-26 | Ucb Biopharma Sprl | Therapeutic agents |
| KR20200116481A (ko) | 2018-01-29 | 2020-10-12 | 메르크 파텐트 게엠베하 | Gcn2 억제제 및 이의 용도 |
| SG11202006832YA (en) | 2018-01-29 | 2020-08-28 | Merck Patent Gmbh | Gcn2 inhibitors and uses thereof |
| AU2019217870A1 (en) * | 2018-02-07 | 2020-08-27 | Insmed Incorporated | Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating ANCA associated vasculitides |
| JP7220204B2 (ja) * | 2018-03-27 | 2023-02-09 | 本田技研工業株式会社 | フッ化物イオン二次電池用正極活物質、当該活物質を用いた正極、およびフッ化物イオン二次電池、並びに当該活物質の製造方法 |
| WO2019204354A1 (en) | 2018-04-16 | 2019-10-24 | C4 Therapeutics, Inc. | Spirocyclic compounds |
| EP3556760A1 (en) * | 2018-04-19 | 2019-10-23 | F. Hoffmann-La Roche AG | Spiro compounds |
| EP3578561A1 (en) * | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| KR102659126B1 (ko) | 2022-03-24 | 2024-04-19 | 충남대학교산학협력단 | 항결핵 약학조성물 |
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| GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| IL125686A (en) | 1996-02-13 | 2002-11-10 | Zeneca Ltd | Quinazoline derivatives, processes for their preparation, pharmaceutical preparations containing them and their use in the manufacture of a drug with an anti-angiogenic effect and / or an effect of reducing vascular permeability |
| DE69709319T2 (de) | 1996-03-05 | 2002-08-14 | Astrazeneca Ab | 4-anilinochinazolin derivate |
| GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
| GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
| GB9900752D0 (en) | 1999-01-15 | 1999-03-03 | Angiogene Pharm Ltd | Benzimidazole vascular damaging agents |
| CN1431999A (zh) | 2000-05-31 | 2003-07-23 | 阿斯特拉曾尼卡有限公司 | 具有血管损伤活性的吲哚衍生物 |
| MXPA02012903A (es) | 2000-07-07 | 2004-07-30 | Angiogene Pharm Ltd | Derivados de colquinol como inhibidores de angiogenesis. |
| CN1255391C (zh) | 2000-07-07 | 2006-05-10 | 安吉奥金尼药品有限公司 | 作为血管破坏剂的colchinol衍生物 |
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| KR20170051521A (ko) | 2008-04-16 | 2017-05-11 | 포톨라 파마슈티컬스, 인코포레이티드 | ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드 |
| JP5512665B2 (ja) * | 2008-06-20 | 2014-06-04 | ジェネンテック， インコーポレイテッド | トリアゾロピリジンｊａｋ阻害剤化合物と方法 |
| WO2010010184A1 (en) * | 2008-07-25 | 2010-01-28 | Galapagos Nv | [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
| EP2438066A2 (en) * | 2009-06-05 | 2012-04-11 | Cephalon, Inc. | PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a]PYRIDINE DERIVATIVES |
| EP2454239B1 (en) * | 2009-07-15 | 2014-08-13 | Janssen Pharmaceuticals Inc. | Substituted triazole and imidazole derivatives as gamma secretase modulators |
| BR112012017310A2 (pt) | 2010-01-15 | 2016-04-19 | Janssen Pharmaceuticals Inc | derivados de triazol substituídos como moduladores de gama secretase |
| US20110190269A1 (en) * | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
| US8486967B2 (en) * | 2010-02-17 | 2013-07-16 | Hoffmann-La Roche Inc. | Heteroaryl substituted piperidines |
| JP4940370B2 (ja) * | 2010-06-29 | 2012-05-30 | キヤノン株式会社 | 電子写真感光体、プロセスカートリッジおよび電子写真装置 |
| MX2013002198A (es) | 2010-08-27 | 2013-03-18 | Merck Patent Gmbh | Derivados de triazolopirazina. |
| ES2674451T3 (es) * | 2012-02-21 | 2018-06-29 | Merck Patent Gmbh | 2-amino-[1,2,4]triazolo[1,5-a] pirazinas 8-sustituidos como inhibidores de la SYK tirosina quinasa e inhibidores de la serina quinasa GCN2 |
-
2013
- 2013-01-22 ES ES13700849.6T patent/ES2674451T3/es active Active
- 2013-01-22 WO PCT/EP2013/000189 patent/WO2013124026A1/en active Application Filing
- 2013-01-22 US US14/379,316 patent/US9120804B2/en active Active
- 2013-01-22 AU AU2013224421A patent/AU2013224421B2/en active Active
- 2013-01-22 EP EP13700849.6A patent/EP2817310B1/en active Active
- 2013-01-22 JP JP2014558028A patent/JP6479476B2/ja active Active
- 2013-01-22 CA CA2863723A patent/CA2863723C/en active Active
- 2013-01-22 CN CN201380010357.1A patent/CN104114557B/zh active Active
- 2013-02-20 TW TW102105907A patent/TW201339165A/zh unknown
- 2013-02-21 AR ARP130100517A patent/AR090104A1/es unknown
-
2014
- 2014-08-06 IL IL233982A patent/IL233982A/en active IP Right Grant
-
2017
- 2017-09-08 JP JP2017173002A patent/JP2018039805A/ja not_active Withdrawn
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