JP2013511547A5 - - Google Patents
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- Publication number
- JP2013511547A5 JP2013511547A5 JP2012540093A JP2012540093A JP2013511547A5 JP 2013511547 A5 JP2013511547 A5 JP 2013511547A5 JP 2012540093 A JP2012540093 A JP 2012540093A JP 2012540093 A JP2012540093 A JP 2012540093A JP 2013511547 A5 JP2013511547 A5 JP 2013511547A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- compound
- pharmaceutical composition
- autoimmune
- cell
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 35
- 150000003839 salts Chemical class 0.000 claims description 35
- 238000000034 method Methods 0.000 claims description 27
- 239000008194 pharmaceutical composition Substances 0.000 claims description 26
- 208000023275 Autoimmune disease Diseases 0.000 claims description 15
- 230000002401 inhibitory effect Effects 0.000 claims description 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 102000000551 Syk Kinase Human genes 0.000 claims description 11
- 108010016672 Syk Kinase Proteins 0.000 claims description 11
- 102000009109 Fc receptors Human genes 0.000 claims description 9
- 108010087819 Fc receptors Proteins 0.000 claims description 9
- 201000010099 disease Diseases 0.000 claims description 8
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 8
- 230000001363 autoimmune Effects 0.000 claims description 6
- 230000001419 dependent effect Effects 0.000 claims description 6
- 102000005962 receptors Human genes 0.000 claims description 6
- 108020003175 receptors Proteins 0.000 claims description 6
- 230000019491 signal transduction Effects 0.000 claims description 6
- 230000000694 effects Effects 0.000 claims description 5
- 206010061218 Inflammation Diseases 0.000 claims description 4
- 208000035269 cancer or benign tumor Diseases 0.000 claims description 4
- 201000001981 dermatomyositis Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 230000004054 inflammatory process Effects 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 231100000241 scar Toxicity 0.000 claims description 4
- 210000001519 tissue Anatomy 0.000 claims description 4
- 208000004300 Atrophic Gastritis Diseases 0.000 claims description 2
- 206010050245 Autoimmune thrombocytopenia Diseases 0.000 claims description 2
- 208000023328 Basedow disease Diseases 0.000 claims description 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 2
- 208000008720 Bone Marrow Neoplasms Diseases 0.000 claims description 2
- 206010008909 Chronic Hepatitis Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical class [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims description 2
- 208000036495 Gastritis atrophic Diseases 0.000 claims description 2
- 208000024869 Goodpasture syndrome Diseases 0.000 claims description 2
- 208000015023 Graves' disease Diseases 0.000 claims description 2
- 208000001204 Hashimoto Disease Diseases 0.000 claims description 2
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims description 2
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims description 2
- 206010019755 Hepatitis chronic active Diseases 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 2
- 102000009438 IgE Receptors Human genes 0.000 claims description 2
- 108010073816 IgE Receptors Proteins 0.000 claims description 2
- 102000009490 IgG Receptors Human genes 0.000 claims description 2
- 108010073807 IgG Receptors Proteins 0.000 claims description 2
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical class [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 206010034277 Pemphigoid Diseases 0.000 claims description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical class [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 2
- 208000033464 Reiter syndrome Diseases 0.000 claims description 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 2
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical class [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims description 2
- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims description 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims description 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims description 2
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 241000700605 Viruses Species 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 150000003863 ammonium salts Chemical class 0.000 claims description 2
- 208000007502 anemia Diseases 0.000 claims description 2
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims description 2
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims description 2
- 229940077388 benzenesulfonate Drugs 0.000 claims description 2
- 201000006491 bone marrow cancer Diseases 0.000 claims description 2
- 208000000594 bullous pemphigoid Diseases 0.000 claims description 2
- 159000000007 calcium salts Chemical class 0.000 claims description 2
- 208000016644 chronic atrophic gastritis Diseases 0.000 claims description 2
- 230000006378 damage Effects 0.000 claims description 2
- SMBQBQBNOXIFSF-UHFFFAOYSA-N dilithium Chemical class [Li][Li] SMBQBQBNOXIFSF-UHFFFAOYSA-N 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- KCIDZIIHRGYJAE-YGFYJFDDSA-L dipotassium;[(2r,3r,4s,5r,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] phosphate Chemical class [K+].[K+].OC[C@H]1O[C@H](OP([O-])([O-])=O)[C@H](O)[C@@H](O)[C@H]1O KCIDZIIHRGYJAE-YGFYJFDDSA-L 0.000 claims description 2
- 201000002491 encephalomyelitis Diseases 0.000 claims description 2
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims description 2
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims description 2
- 238000000099 in vitro assay Methods 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 159000000003 magnesium salts Chemical class 0.000 claims description 2
- 230000003211 malignant effect Effects 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 206010028417 myasthenia gravis Diseases 0.000 claims description 2
- 201000005737 orchitis Diseases 0.000 claims description 2
- 210000000056 organ Anatomy 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 208000002574 reactive arthritis Diseases 0.000 claims description 2
- 210000002966 serum Anatomy 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 230000009885 systemic effect Effects 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims description 2
- 238000000338 in vitro Methods 0.000 claims 4
- 208000032544 Cicatrix Diseases 0.000 claims 2
- 230000037387 scars Effects 0.000 claims 2
- 230000001105 regulatory effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26316909P | 2009-11-20 | 2009-11-20 | |
| US61/263,169 | 2009-11-20 | ||
| PCT/US2010/057442 WO2011063241A1 (en) | 2009-11-20 | 2010-11-19 | 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013511547A JP2013511547A (ja) | 2013-04-04 |
| JP2013511547A5 true JP2013511547A5 (enExample) | 2014-01-16 |
| JP5681723B2 JP5681723B2 (ja) | 2015-03-11 |
Family
ID=43430840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012540093A Expired - Fee Related JP5681723B2 (ja) | 2009-11-20 | 2010-11-19 | ２，４−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US8389515B2 (enExample) |
| EP (1) | EP2501705B1 (enExample) |
| JP (1) | JP5681723B2 (enExample) |
| CA (1) | CA2780777C (enExample) |
| ES (1) | ES2524127T3 (enExample) |
| WO (1) | WO2011063241A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011044545A2 (en) | 2009-10-09 | 2011-04-14 | Sigalov Alexander B | Methods and compositions for targeted imaging |
| EP2501705B1 (en) | 2009-11-20 | 2014-08-27 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses |
| JP6067550B2 (ja) * | 2010-04-13 | 2017-01-25 | 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 | ２，４−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 |
| SMT201900071T1 (it) | 2011-07-28 | 2019-02-28 | Rigel Pharmaceuticals Inc | Nuove formulazioni di (trimetossifenilammino)pirimidinile |
| WO2013130354A1 (en) * | 2012-02-29 | 2013-09-06 | University Hospitals Cleveland Medical Center | Targeted treatment of anerobic cancer |
| WO2013189241A1 (zh) * | 2012-06-20 | 2013-12-27 | 上海恒瑞医药有限公司 | 嘧啶二胺类衍生物、其制备方法及其在医药上的应用 |
| RU2519546C1 (ru) * | 2013-01-16 | 2014-06-10 | Общество С Ограниченной Ответственностью "Биоинтегратор" (Ооо "Биоинтегратор") | КОНЪЮГАТЫ И МАЛЫЕ МОЛЕКУЛЫ, ВЗАИМОДЕЙСТВУЮЩИЕ С РЕЦЕПТОРОМ CD16а |
| CA3186267C (en) * | 2013-12-20 | 2025-09-09 | Rigel Pharmaceuticals, Inc. | PHARMACEUTICAL PROCESS AND INTERMEDIARIES |
| US10981951B2 (en) | 2014-01-31 | 2021-04-20 | Mayo Foundation For Medical Education And Research | Therapeutics for the treatment of glaucoma |
| EP4072543A4 (en) | 2019-12-12 | 2024-02-07 | Qlaris Bio, Inc. | CONTROLLED RELEASE CROMAKALIM PRODRUGS |
| WO2022175829A1 (en) * | 2021-02-17 | 2022-08-25 | Cellix Bio Private Limited | Topical formulations and compositions |
| US20250017895A1 (en) * | 2021-11-29 | 2025-01-16 | The Children's Hospital Of Philadelphia | Flavanoid containing compositions and methods of use thereof for the treatment of mitochondrial disorders |
| CN119431398A (zh) * | 2023-07-31 | 2025-02-14 | 中国科学院上海有机化学研究所 | R406及其衍生物协同trail的抗肿瘤应用 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6573256B2 (en) | 1996-12-30 | 2003-06-03 | Bone Care International, Inc. | Method of inhibiting angiogenesis using active vitamin D analogues |
| FR2785284B1 (fr) | 1998-11-02 | 2000-12-01 | Galderma Res & Dev | Analogues de la vitamine d |
| US6358939B1 (en) | 1999-12-21 | 2002-03-19 | Northern Lights Pharmaceuticals, Llc | Use of biologically active vitamin D compounds for the prevention and treatment of inflammatory bowel disease |
| US6924400B2 (en) | 2001-12-10 | 2005-08-02 | Galderma Research & Development, Snc | Triaromatic vitamin D analogues |
| US6849245B2 (en) * | 2001-12-11 | 2005-02-01 | Catalytic Materials Llc | Catalysts for producing narrow carbon nanostructures |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| IL166241A0 (en) * | 2002-07-29 | 2006-01-15 | Rigel Pharmaceuticals Inc | Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds |
| US20060160834A1 (en) | 2003-06-06 | 2006-07-20 | Fong Tung M | Combination therapy for the treatment of hypertension |
| ES2421139T3 (es) * | 2003-07-30 | 2013-08-29 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias |
| DK1663242T3 (da) * | 2003-08-07 | 2011-08-01 | Rigel Pharmaceuticals Inc | 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler |
| US20070092888A1 (en) | 2003-09-23 | 2007-04-26 | Cornelius Diamond | Diagnostic markers of hypertension and methods of use thereof |
| US7449458B2 (en) * | 2005-01-19 | 2008-11-11 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| US8227455B2 (en) * | 2005-04-18 | 2012-07-24 | Rigel Pharmaceuticals, Inc. | Methods of treating cell proliferative disorders |
| US7713987B2 (en) * | 2005-12-06 | 2010-05-11 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2,4-diamines and their uses |
| JP2008013527A (ja) * | 2006-07-10 | 2008-01-24 | Sankyo Co Ltd | チエノ［３，２−ｄ］ピリミジン−２，４−ジアミン誘導体 |
| WO2008064274A1 (en) | 2006-11-21 | 2008-05-29 | Rigel Pharmaceuticals, Inc. | Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses |
| EP2382210B1 (en) * | 2008-12-30 | 2017-03-01 | Rigel Pharmaceuticals, Inc. | Pyrimidinediamine kinase inhibitors |
| EP2501705B1 (en) | 2009-11-20 | 2014-08-27 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses |
-
2010
- 2010-11-19 EP EP10782509.3A patent/EP2501705B1/en not_active Not-in-force
- 2010-11-19 WO PCT/US2010/057442 patent/WO2011063241A1/en not_active Ceased
- 2010-11-19 CA CA2780777A patent/CA2780777C/en active Active
- 2010-11-19 ES ES10782509.3T patent/ES2524127T3/es active Active
- 2010-11-19 JP JP2012540093A patent/JP5681723B2/ja not_active Expired - Fee Related
- 2010-11-19 US US12/950,612 patent/US8389515B2/en not_active Expired - Fee Related
-
2013
- 2013-02-05 US US13/759,457 patent/US8642593B2/en not_active Expired - Fee Related
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