JP2014508780A5 - - Google Patents
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- JP2014508780A5 JP2014508780A5 JP2013557916A JP2013557916A JP2014508780A5 JP 2014508780 A5 JP2014508780 A5 JP 2014508780A5 JP 2013557916 A JP2013557916 A JP 2013557916A JP 2013557916 A JP2013557916 A JP 2013557916A JP 2014508780 A5 JP2014508780 A5 JP 2014508780A5
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- 239000000203 mixture Substances 0.000 claims 22
- 210000003491 Skin Anatomy 0.000 claims 7
- 206010039710 Scleroderma Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000011780 sodium chloride Substances 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 4
- RSNPAKAFCAAMBH-UHFFFAOYSA-N 3-(5-amino-2-methyl-4-oxoquinazolin-3-yl)piperidine-2,6-dione Chemical compound CC1=NC2=CC=CC(N)=C2C(=O)N1C1CCC(=O)NC1=O RSNPAKAFCAAMBH-UHFFFAOYSA-N 0.000 claims 3
- -1 5-amino-2-methyl-4-oxoquinazolin-3 (4H) -yl Chemical group 0.000 claims 3
- 208000000059 Dyspnea Diseases 0.000 claims 3
- 206010013975 Dyspnoeas Diseases 0.000 claims 3
- 208000006820 Arthralgia Diseases 0.000 claims 2
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- 210000003414 Extremities Anatomy 0.000 claims 2
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- 208000003251 Pruritus Diseases 0.000 claims 2
- 206010037912 Raynaud's phenomenon Diseases 0.000 claims 2
- 206010068760 Ulcers Diseases 0.000 claims 2
- 201000004384 alopecia Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
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- 231100000862 numbness Toxicity 0.000 claims 2
- 239000007787 solid Chemical group 0.000 claims 2
- 201000009594 systemic scleroderma Diseases 0.000 claims 2
- 231100000397 ulcer Toxicity 0.000 claims 2
- XGWFJBFNAQHLEF-UHFFFAOYSA-N 9-anthroic acid Chemical compound C1=CC=C2C(C(=O)O)=C(C=CC=C3)C3=CC2=C1 XGWFJBFNAQHLEF-UHFFFAOYSA-N 0.000 claims 1
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 108010022043 Antineutrophil Cytoplasmic Antibodies Proteins 0.000 claims 1
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 1
- 206010002855 Anxiety Diseases 0.000 claims 1
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- 201000002829 CREST syndrome Diseases 0.000 claims 1
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- 206010010774 Constipation Diseases 0.000 claims 1
- 208000000264 Deglutition Disorders Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 206010013082 Discomfort Diseases 0.000 claims 1
- 206010013950 Dysphagia Diseases 0.000 claims 1
- 210000001513 Elbow Anatomy 0.000 claims 1
- 206010015037 Epilepsy Diseases 0.000 claims 1
- 208000010201 Exanthema Diseases 0.000 claims 1
- 210000001145 Finger Joint Anatomy 0.000 claims 1
- 210000001035 Gastrointestinal Tract Anatomy 0.000 claims 1
- KNCYXPMJDCCGSJ-UHFFFAOYSA-N Glutarimide Chemical compound O=C1CCCC(=O)N1 KNCYXPMJDCCGSJ-UHFFFAOYSA-N 0.000 claims 1
- 206010019233 Headache Diseases 0.000 claims 1
- 208000000616 Hemoptysis Diseases 0.000 claims 1
- 208000002551 Irritable Bowel Syndrome Diseases 0.000 claims 1
- 206010023230 Joint stiffness Diseases 0.000 claims 1
- 206010023232 Joint swelling Diseases 0.000 claims 1
- 210000001503 Joints Anatomy 0.000 claims 1
- 206010024648 Livedo reticularis Diseases 0.000 claims 1
- 208000008771 Lymphadenopathy Diseases 0.000 claims 1
- 206010025482 Malaise Diseases 0.000 claims 1
- 206010028417 Myasthenia gravis Diseases 0.000 claims 1
- 206010028813 Nausea Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010034719 Personality change Diseases 0.000 claims 1
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- 206010037660 Pyrexia Diseases 0.000 claims 1
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- 206010040767 Sjogren's syndrome Diseases 0.000 claims 1
- 206010040829 Skin discolouration Diseases 0.000 claims 1
- 206010042674 Swelling Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 238000002266 amputation Methods 0.000 claims 1
- 230000003110 anti-inflammatory Effects 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- UGFAIRIUMAVXCW-UHFFFAOYSA-N carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 claims 1
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 230000001419 dependent Effects 0.000 claims 1
- 201000008286 diarrhea Diseases 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 230000002496 gastric Effects 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 230000002519 immonomodulatory Effects 0.000 claims 1
- 200000000018 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000004199 lung function Effects 0.000 claims 1
- 230000002093 peripheral Effects 0.000 claims 1
- 230000000241 respiratory Effects 0.000 claims 1
- 230000029058 respiratory gaseous exchange Effects 0.000 claims 1
- 230000033764 rhythmic process Effects 0.000 claims 1
- 230000037370 skin discoloration Effects 0.000 claims 1
- 231100000046 skin rash Toxicity 0.000 claims 1
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- 230000024883 vasodilation Effects 0.000 claims 1
- 230000000261 vasodilator Effects 0.000 claims 1
- 239000003071 vasodilator agent Substances 0.000 claims 1
- 230000000007 visual effect Effects 0.000 claims 1
Claims (14)
- 免疫関連疾患又は炎症性疾患を治療する、予防する、又は管理するための医薬組成物であって、有効量の3-(5-アミノ-2-メチル-4-オキソキナゾリン-3(4H)-イル)ピペリジン-2,6-ジオン、又はその医薬として許容し得る塩、溶媒和化合物、水和物、立体異性体、互変異性体、ラセミ混合物、共結晶、クラスレート、若しくは多形体を含む、前記組成物。
- 前記疾患が、全身性エリテマトーデス、強皮症、シェーグレン症候群、ANCA誘導型血管炎、抗リン脂質抗体症候群、又は重症筋無力症である、請求項１記載の組成物。
- 前記疾患が、全身性エリテマトーデスである、請求項１又は２記載の組成物。
- 前記疾患が、重篤な全身性エリテマトーデスである、請求項１から３のいずれか一項記載の組成物。
- 前記疾患が、強皮症である、請求項１又は２記載の組成物。
- 前記強皮症が、限局性、全身性、限局型全身性、又は汎発性強皮症である、請求項５記載の組成物。
- 前記全身性強皮症が、CREST症候群を含む、請求項６記載の組成物。
- 全身性エリテマトーデスの症状を軽減する、抑制する、又は予防するための医薬組成物であって、有効量の3-(5-アミノ-2-メチル-4-オキソキナゾリン-3(4H)-イル)ピペリジン-2,6-ジオン、又はその医薬として許容し得る塩、溶媒和化合物、水和物、立体異性体、互変異性体、若しくはラセミ混合物を含み、該症状が、関節の痛み、関節の腫脹、関節炎、深呼吸時の胸痛、倦怠感、他に原因のない発熱、全身違和感、不安、脱毛、口の糜爛、リンパ節腫脹、日光過敏、皮疹、頭痛、しびれ、刺痛、てんかん発作、視覚問題、人格変化、腹痛、悪心、嘔吐、心拍リズム異常、喀血及び呼吸困難、斑状の皮膚色、及びレイノー現象からなる群から選択される、前記組成物。
- 強皮症の症状を軽減する、抑制する、又は予防するための医薬組成物であって、有効量の3-(5-アミノ-2-メチル-4-オキソキナゾリン-3(4H)-イル)ピペリジン-2,6-ジオン、又はその医薬として許容し得る塩、溶媒和化合物、水和物、立体異性体、互変異性体、ラセミ混合物、共結晶、クラスレート、若しくは多形体を含み、該症状が、(i)皮膚の漸進的な硬化、肥厚、及びこわばり;(ii)皮膚変色;(iii)四肢のしびれ;(iv)皮膚の光沢;(v)白墨のように白い流体が噴出する、皮膚の表面下の小さな白色の塊;(vi) レイノー性食道機能異常;(vii)末梢血管拡張;(viii)関節の痛み及び/又は硬直;(ix)手足の腫脹;(x)皮膚の痒み;(xi)指の硬直及び湾曲;(xii)指関節及び肘などのある種の関節の外側の潰瘍;(xiii)消化管異常、例えば、胸やけ、嚥下困難、下痢、過敏性腸、及び便秘;(xiv)倦怠感及び脱力感;(xv)息切れ;(xvi) 関節炎;(xvii)脱毛;(xviii)内臓異常;(xix)指潰瘍;及び(xx)手指の自然切断からなる群から選択される、前記組成物。
- 強皮症に罹患する患者の、修正Rodnanスキンスコアを向上させる、皮膚厚を減少若しくは改善させる、皮膚硬化を減少若しくは改善させる、肺機能を改善する、皮膚科学的生活の質指標を改善する、一酸化炭素拡散能を改善する、Mahler呼吸困難指数を改善する、Saint Georgeの呼吸器質問票スコアを改善する、UCLA強皮症臨床試験コンソーシアム消化管スコアを改善する、流量依存性血管拡張反応を改善する、6分間歩行距離を改善若しくは増大させるための医薬組成物であって、有効量の3-(5-アミノ-2-メチル-4-オキソキナゾリン-3(4H)-イル)ピペリジン-2,6-ジオン、又はその医薬として許容し得る塩、溶媒和化合物、水和物、立体異性体、互変異性体、ラセミ混合物、共結晶、クラスレート、若しくは多形体を含む、前記組成物。
- 第2の活性剤と組合せて投与され、該第2の活性剤が、抗炎症又は免疫調節化合物である、請求項１から１０のいずれか一項記載の組成物。
- 前記有効量が、約0.005mg/kgから約10mg/kg(患者の体重)である、請求項１から１１のいずれか一項記載の組成物。
- B細胞の活性を調節するための組成物であって、該細胞を、有効量の3-(5-アミノ-2-メチル-4-オキソキナゾリン-3(4H)-イル)ピペリジン-2,6-ジオン、又はその医薬として許容し得る塩、固体形、溶媒和化合物、水和物、立体異性体、互変異性体、ラセミ混合物、共結晶、クラスレート、若しくは多形体と接触させることを含む、前記組成物。
- T細胞の活性を調節するための組成物であって、該細胞を、有効量の3-(5-アミノ-2-メチル-4-オキソキナゾリン-3(4H)-イル)ピペリジン-2,6-ジオン、又はその医薬として許容し得る塩、固体形、溶媒和化合物、水和物、互変異性体、立体異性体、ラセミ混合物、共結晶、クラスレート、若しくは多形体と接触させることを含む、前記組成物。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161451995P | 2011-03-11 | 2011-03-11 | |
| US61/451,995 | 2011-03-11 | ||
| US201161480272P | 2011-04-28 | 2011-04-28 | |
| US61/480,272 | 2011-04-28 | ||
| PCT/US2012/028538 WO2012125475A1 (en) | 2011-03-11 | 2012-03-09 | Use of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4h)-yl)piperidine-2-6-dione in treatment of immune-related and inflammatory diseases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016248598A Division JP2017081959A (ja) | 2011-03-11 | 2016-12-22 | 免疫関連疾患及び炎症性疾患の治療における３−（５−アミノ−２−メチル−４−オキソキナゾリン−３（４ｈ）−イル）ピペリジン−２，６−ジオンの使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014508780A JP2014508780A (ja) | 2014-04-10 |
| JP2014508780A5 true JP2014508780A5 (ja) | 2015-04-23 |
| JP6118273B2 JP6118273B2 (ja) | 2017-04-19 |
Family
ID=45876915
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013557916A Expired - Fee Related JP6118273B2 (ja) | 2011-03-11 | 2012-03-09 | 免疫関連疾患及び炎症性疾患の治療における３−（５−アミノ−２−メチル−４−オキソキナゾリン−３（４ｈ）−イル）ピペリジン−２，６−ジオンの使用 |
| JP2013557904A Withdrawn JP2014510078A (ja) | 2011-03-11 | 2012-03-09 | ３−（５−アミノ−２−メチル−４−オキソ−４ｈ−キナゾリン−３−イル）−ピペリジン−２，６−ジオンを用いる癌の治療方法 |
| JP2016248598A Pending JP2017081959A (ja) | 2011-03-11 | 2016-12-22 | 免疫関連疾患及び炎症性疾患の治療における３−（５−アミノ−２−メチル−４−オキソキナゾリン−３（４ｈ）−イル）ピペリジン−２，６−ジオンの使用 |
| JP2017009923A Expired - Fee Related JP6348192B2 (ja) | 2011-03-11 | 2017-01-24 | ３−（５−アミノ−２−メチル−４−オキソ−４ｈ−キナゾリン−３−イル）−ピペリジン−２，６−ジオンを用いる癌の治療方法 |
| JP2018103019A Withdrawn JP2018168159A (ja) | 2011-03-11 | 2018-05-30 | ３−（５−アミノ−２−メチル−４−オキソ−４ｈ−キナゾリン−３−イル）−ピペリジン−２，６−ジオンを用いる癌の治療方法 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013557904A Withdrawn JP2014510078A (ja) | 2011-03-11 | 2012-03-09 | ３−（５−アミノ−２−メチル−４−オキソ−４ｈ−キナゾリン−３−イル）−ピペリジン−２，６−ジオンを用いる癌の治療方法 |
| JP2016248598A Pending JP2017081959A (ja) | 2011-03-11 | 2016-12-22 | 免疫関連疾患及び炎症性疾患の治療における３−（５−アミノ−２−メチル−４−オキソキナゾリン−３（４ｈ）−イル）ピペリジン−２，６−ジオンの使用 |
| JP2017009923A Expired - Fee Related JP6348192B2 (ja) | 2011-03-11 | 2017-01-24 | ３−（５−アミノ−２−メチル−４−オキソ−４ｈ−キナゾリン−３−イル）−ピペリジン−２，６−ジオンを用いる癌の治療方法 |
| JP2018103019A Withdrawn JP2018168159A (ja) | 2011-03-11 | 2018-05-30 | ３−（５−アミノ−２−メチル−４−オキソ−４ｈ−キナゾリン−３−イル）−ピペリジン−２，６−ジオンを用いる癌の治療方法 |
Country Status (29)
| Country | Link |
|---|---|
| US (6) | US20140148473A1 (ja) |
| EP (3) | EP3025715A1 (ja) |
| JP (5) | JP6118273B2 (ja) |
| KR (2) | KR20140019364A (ja) |
| CN (3) | CN103561744A (ja) |
| AR (1) | AR085651A1 (ja) |
| AU (4) | AU2012229316B2 (ja) |
| BR (2) | BR112013023277A2 (ja) |
| CA (2) | CA2829592A1 (ja) |
| CY (1) | CY1117430T1 (ja) |
| DK (1) | DK2683384T3 (ja) |
| EA (2) | EA201691939A1 (ja) |
| ES (2) | ES2659205T3 (ja) |
| HK (1) | HK1191858A1 (ja) |
| HR (1) | HRP20160056T1 (ja) |
| HU (1) | HUE027481T2 (ja) |
| IL (2) | IL227990B (ja) |
| MX (2) | MX2013010153A (ja) |
| NI (2) | NI201300082A (ja) |
| PL (1) | PL2683384T3 (ja) |
| PT (1) | PT2683384E (ja) |
| RS (1) | RS54553B1 (ja) |
| RU (3) | RU2013145556A (ja) |
| SG (2) | SG193320A1 (ja) |
| SI (1) | SI2683384T1 (ja) |
| SM (1) | SMT201600034B (ja) |
| TW (2) | TWI542349B (ja) |
| WO (2) | WO2012125475A1 (ja) |
| ZA (2) | ZA201306148B (ja) |
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| CA2829570C (en) | 2011-03-11 | 2019-05-07 | Celgene Corporation | Solid forms of 3-(5-amino-2-methyl-4-oxo-4h-quinazolin-3-yl)-piperidine-2,6-dione, and their pharmaceutical compositions and uses |
| WO2012135299A1 (en) | 2011-03-28 | 2012-10-04 | Deuteria Pharmaceuticals Inc | 2',6'-dioxo-3'-deutero-piperdin-3-yl-isoindoline compounds |
| CN103688176A (zh) * | 2011-04-29 | 2014-03-26 | 细胞基因公司 | 利用cereblon作为预报因子治疗癌和炎性疾病的方法 |
| CA3136093A1 (en) | 2012-06-29 | 2014-01-03 | Celgene Corporation | Methods for determining drug efficacy using cereblon-associated proteins |
| TWI723266B (zh) * | 2012-08-09 | 2021-04-01 | 美商西建公司 | 利用3-(4-((4-(嗎啉基甲基)苄基)氧基)-1-氧異吲哚啉-2-基)六氫吡啶-2,6-二酮治療癌症之方法 |
| US9587281B2 (en) | 2012-08-14 | 2017-03-07 | Celgene Corporation | Cereblon isoforms and their use as biomarkers for therapeutic treatment |
| JP2015531776A (ja) | 2012-09-04 | 2015-11-05 | セルジーン コーポレイション | ３−（５−アミノ−２−メチル−４−オキソキナゾリン−３（４ｈ）−イル）ピペリジン−２，６−ジオンのアイソトポログ及びその製造方法 |
| CN104797256A (zh) * | 2012-09-10 | 2015-07-22 | 细胞基因公司 | 用于治疗局部晚期乳腺癌的方法 |
| AU2014205043B2 (en) | 2013-01-14 | 2018-10-04 | Deuterx, Llc | 3-(5-substituted-4-oxoquinazolin-3(4h)-yl)-3-deutero-piperidine-2,6-dione derivatives |
| WO2014152833A1 (en) | 2013-03-14 | 2014-09-25 | Deuterx, Llc | 3-(substituted-4-oxo-quinazolin-3(4h)-yl)-3-deutero-piperidine-2,6-dione derivatives |
| CA2909625C (en) * | 2013-04-17 | 2021-06-01 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| EP2986321A1 (en) * | 2013-04-17 | 2016-02-24 | Signal Pharmaceuticals, LLC | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| NZ628322A (en) * | 2013-05-01 | 2017-06-30 | Celgene Corp | Synthesis of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4h)-yl)piperidine-2,6-dione |
| WO2014179661A1 (en) | 2013-05-03 | 2014-11-06 | Celgene Corporation | Methods for treating cancer using combination therapy |
| US20160282354A1 (en) | 2013-11-08 | 2016-09-29 | The Broad Institute, Inc. | Compositions and methods for selecting a treatment for b-cell neoplasias |
| CA3206268A1 (en) * | 2013-12-06 | 2015-06-11 | Celgene Corporation | Methods for determining drug efficacy for the treatment of diffuse large b-cell lymphoma, multiple myeloma, and myeloid cancers |
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