JP2013518882A5 - - Google Patents
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- JP2013518882A5 JP2013518882A5 JP2012551997A JP2012551997A JP2013518882A5 JP 2013518882 A5 JP2013518882 A5 JP 2013518882A5 JP 2012551997 A JP2012551997 A JP 2012551997A JP 2012551997 A JP2012551997 A JP 2012551997A JP 2013518882 A5 JP2013518882 A5 JP 2013518882A5
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- pharmaceutically acceptable
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- medicament
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- 150000001875 compounds Chemical class 0.000 claims 11
- 239000003814 drug Substances 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 230000037396 body weight Effects 0.000 claims 6
- -1 3-methoxy-1,2,4-thiadiazol-5-yl Chemical group 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 201000008937 atopic dermatitis Diseases 0.000 claims 3
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 241001465754 Metazoa Species 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- UGUHFDPGDQDVGX-UHFFFAOYSA-N 1,2,3-thiadiazole Chemical group C1=CSN=N1 UGUHFDPGDQDVGX-UHFFFAOYSA-N 0.000 claims 1
- 125000004521 1,3,4-thiadiazol-2-yl group Chemical group S1C(=NN=C1)* 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000014085 Chronic respiratory disease Diseases 0.000 claims 1
- 206010012434 Dermatitis allergic Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 230000002917 arthritic effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010023332 keratitis Diseases 0.000 claims 1
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 1
- 244000144972 livestock Species 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- JSPCTNUQYWIIOT-UHFFFAOYSA-N piperidine-1-carboxamide Chemical compound NC(=O)N1CCCCC1 JSPCTNUQYWIIOT-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 0 CN(C1NCN=C2NC=CC12)[C@@](C1)C(*)CCN1C(N*)=O Chemical compound CN(C1NCN=C2NC=CC12)[C@@](C1)C(*)CCN1C(N*)=O 0.000 description 1
Claims (17)
- 式Ｉの化合物：
- 式ＩＡの化合物
- Ｒ１が、メチルである、請求項１または２に記載の化合物または薬学的に許容できるその塩。
- Ｒ２が、１，３，４−チアジアゾール−２−イルである、請求項１または２に記載の化合物または薬学的に許容できるその塩。
- Ｒ２が、３−メトキシ−１，２，４−チアジアゾール−５−イルである、請求項１または２に記載の化合物または薬学的に許容できるその塩。
- （３Ｒ，４Ｒ）−４−メチル−３−［メチル（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）アミノ］−Ｎ−（１，３，４−チアジアゾール−２−イル）ピペリジン−１−カルボキサミドである、請求項１に記載の化合物または薬学的に許容できるその塩。
- （３Ｒ，４Ｒ）−Ｎ−（３−メトキシ−１，２，４−チアジアゾール−５−イル）−４−メチル−３−［メチル（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）アミノ］ピペリジン−１−カルボキサミドである、請求項１に記載の化合物または薬学的に許容できるその塩。
- 請求項１〜７のいずれか１項に記載の化合物、または薬学的に許容できるその塩、および薬学的に許容できる担体を含む医薬組成物。
- 哺乳動物におけるアレルギー反応、アレルギー性皮膚炎、アトピー性皮膚炎、湿疹、またはそう痒症を治療するための医薬であって、治療有効量の請求項１〜７のいずれか１項に記載の化合物または薬学的に許容できるその塩を含む医薬。
- 前記治療有効量が、０．０１ｍｇ／ｋｇ体重／日〜１００ｍｇ／ｋｇ体重／日である、請求項９に記載の医薬。
- 前記治療有効量が、０．１ｍｇ／ｋｇ体重／日〜１０ｍｇ／ｋｇ体重／日である、請求項９に記載の医薬。
- 前記治療有効量が、０．２ｍｇ／ｋｇ体重／日〜１．５ｍｇ／ｋｇ体重／日である、請求項９に記載の医薬。
- 前記哺乳動物が、愛玩動物を含む、請求項９に記載の医薬。
- 前記愛玩動物が、イヌである、請求項１３に記載の医薬。
- 前記哺乳動物が、家畜を含む、請求項９に記載の医薬。
- 経口、非経口、または局所的に投与される、請求項９に記載の医薬。
- 哺乳動物における神経変性疾患、角結膜炎、慢性呼吸器疾患、自己免疫疾患、炎症性腸疾患、新形成、および関節炎状態を治療するための医薬であって、治療有効量の請求項１〜７のいずれか１項に記載の化合物または薬学的に許容できるその塩を含む医薬。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30191510P | 2010-02-05 | 2010-02-05 | |
| US61/301,915 | 2010-02-05 | ||
| PCT/US2011/022216 WO2011097087A1 (en) | 2010-02-05 | 2011-01-24 | Pyrrolo [ 2, 3 - d] pyrimidine urea compounds as jak inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013518882A JP2013518882A (ja) | 2013-05-23 |
| JP2013518882A5 true JP2013518882A5 (ja) | 2014-03-13 |
Family
ID=43629121
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012551997A Withdrawn JP2013518882A (ja) | 2010-02-05 | 2011-01-24 | ＪＡＫ阻害剤としてのピロロ［２，３−ｄ］ピリミジン尿素化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20120309776A1 (ja) |
| EP (1) | EP2531508A1 (ja) |
| JP (1) | JP2013518882A (ja) |
| CN (1) | CN102822177A (ja) |
| AU (1) | AU2011213198B2 (ja) |
| BR (1) | BR112012019511A2 (ja) |
| CA (1) | CA2788071A1 (ja) |
| MX (1) | MX2012009074A (ja) |
| WO (1) | WO2011097087A1 (ja) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2970354T3 (es) | 2005-12-13 | 2024-05-28 | Incyte Holdings Corp | Derivados de pirrolo[2,3-d]pirimidina como inhibidores de Janus quinasas |
| JP2015528501A (ja) * | 2012-09-12 | 2015-09-28 | ライジェル ファーマシューティカルズ， インコーポレイテッド | 白斑の治療法 |
| KR20210037012A (ko) | 2012-11-15 | 2021-04-05 | 인사이트 홀딩스 코포레이션 | 룩솔리티니브의 서방성 제형 |
| CN103896946B (zh) * | 2012-12-28 | 2018-04-03 | 浙江导明医药科技有限公司 | 用于预防及治疗多种自身免疫疾病的新化合物 |
| WO2014118388A1 (en) | 2013-02-04 | 2014-08-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
| US20140343034A1 (en) * | 2013-04-25 | 2014-11-20 | Japan Tobacco Inc. | Skin barrier function improving agent |
| AU2014277506B2 (en) * | 2013-06-07 | 2017-08-31 | Jiangsu Hengrui Medicine Co., Ltd. | Bisulfate of Janus kinase (JAK) inhibitor and preparation method therefor |
| CN105732637B (zh) * | 2014-12-30 | 2020-04-21 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| WO2017013270A1 (en) | 2015-07-23 | 2017-01-26 | Universite De Strasbourg | Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy |
| KR20180080330A (ko) * | 2015-11-24 | 2018-07-11 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 위장관 염증 질환의 치료를 위한 jak 저해제 화합물의 프로드러그 |
| US10973913B2 (en) * | 2016-02-16 | 2021-04-13 | Washington University | JAK inhibitors and uses thereof |
| WO2018165250A1 (en) | 2017-03-08 | 2018-09-13 | Theravance Biopharma R&D Ip, Llc | Glucuronide prodrugs of tofacitinib |
| WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
| EP3610264A1 (en) | 2017-04-13 | 2020-02-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
| CN110662755A (zh) | 2017-05-23 | 2020-01-07 | 施万生物制药研发Ip有限责任公司 | 托法替尼的硫代氨基甲酸酯前药 |
| CA3063963A1 (en) | 2017-05-23 | 2018-11-29 | Theravance Biopharma R&D Ip, Llc | Glucuronide prodrugs of janus kinase inhibitors |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69531558T2 (de) * | 1995-06-07 | 2004-03-18 | Pfizer Inc. | Heterocyclische kondensierte pyrimidin-derivate |
| RS50087B (sr) | 1998-06-19 | 2009-01-22 | Pfizer Products Inc., | Pirolo (2,3-d) pirimidin jedinjenja |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| PT1235830E (pt) | 1999-12-10 | 2004-04-30 | Pfizer Prod Inc | Compostos de pirrolo¬2,3-d|pirimidina como inibidores das proteina cinases |
| SI1294724T1 (sl) * | 2000-06-26 | 2006-08-31 | Pfizer Prod Inc | Pirolo(2,3-d)primidinske spojine kot imunosupresivna sredstva |
| US7034182B2 (en) * | 2000-06-30 | 2006-04-25 | Elan Pharmaceuticals, Inc. | Compounds to treat Alzheimer's disease |
| US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| JP2006508976A (ja) | 2002-11-21 | 2006-03-16 | ファイザー・プロダクツ・インク | ３−アミノ−ピペラジン誘導体及び製造法 |
| US7732237B2 (en) | 2005-06-27 | 2010-06-08 | The Regents Of The University Of California | Quantum dot based optoelectronic device and method of making same |
| PL1913000T3 (pl) * | 2005-07-29 | 2012-05-31 | Pfizer Prod Inc | Pochodne pirolo[2,3-d]pirymidyny, ich związki pośrednie i synteza |
| WO2008029237A2 (en) * | 2006-09-05 | 2008-03-13 | Pfizer Products Inc. | Combination therapies for rheumatoid arthritis |
-
2011
- 2011-01-24 WO PCT/US2011/022216 patent/WO2011097087A1/en active Application Filing
- 2011-01-24 MX MX2012009074A patent/MX2012009074A/es unknown
- 2011-01-24 AU AU2011213198A patent/AU2011213198B2/en not_active Expired - Fee Related
- 2011-01-24 JP JP2012551997A patent/JP2013518882A/ja not_active Withdrawn
- 2011-01-24 US US13/576,685 patent/US20120309776A1/en not_active Abandoned
- 2011-01-24 CN CN2011800171067A patent/CN102822177A/zh active Pending
- 2011-01-24 EP EP11703762A patent/EP2531508A1/en not_active Withdrawn
- 2011-01-24 BR BR112012019511A patent/BR112012019511A2/pt not_active IP Right Cessation
- 2011-01-24 CA CA2788071A patent/CA2788071A1/en not_active Abandoned
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