IL224869A - History 2 - (aryl / heterocyclic) amino-4,2,1-triazolo [5,1- a] pyrazine sustained in position 8 and drugs containing them - Google Patents
History 2 - (aryl / heterocyclic) amino-4,2,1-triazolo [5,1- a] pyrazine sustained in position 8 and drugs containing themInfo
- Publication number
- IL224869A IL224869A IL224869A IL22486913A IL224869A IL 224869 A IL224869 A IL 224869A IL 224869 A IL224869 A IL 224869A IL 22486913 A IL22486913 A IL 22486913A IL 224869 A IL224869 A IL 224869A
- Authority
- IL
- Israel
- Prior art keywords
- triazolo
- pyrazin
- phenyl
- amine
- hplc purity
- Prior art date
Links
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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| PCT/EP2011/003830 WO2012025186A1 (en) | 2010-08-27 | 2011-07-29 | Triazolopyrazine derivatives |
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| US9120804B2 (en) | 2012-02-21 | 2015-09-01 | Merck Patent Gmbh | 8-substituted 2-amino-[1,2,4] triazolo [1, 5-A] pyrazines as Syk tryrosine kinase inhibitors and GCN2 serin kinase inhibitors |
| JP6049768B2 (ja) * | 2012-03-07 | 2016-12-21 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | トリアゾロピラジン誘導体 |
| EP3550031A1 (en) | 2012-07-24 | 2019-10-09 | Pharmacyclics, LLC | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| BR112015004427A2 (pt) | 2012-10-26 | 2017-07-04 | Hoffmann La Roche | compostos , métodos para o tratamento de um estado inflamatório , da artrite reumatóide , da asma , de um distúrbio imunológico e de um distúrbio imune e composição farmacêutica |
| CA2903901A1 (en) * | 2013-03-05 | 2014-09-12 | Merck Patent Gmbh | 9-(aryl or heteroaryl)-2-(pyrazolyl, pyrrolidinyl or cyclopentyl)aminopurine derivatives as anticancer agents |
| CN105026398B (zh) * | 2013-03-05 | 2018-05-18 | 默克专利股份公司 | 用于治疗疾病诸如癌症的三唑并[4,5-d]嘧啶衍生物 |
| EP2994471B1 (en) * | 2013-05-06 | 2017-05-17 | Merck Patent GmbH | Macrocycles as kinase inhibitors |
| WO2015017402A1 (en) * | 2013-07-29 | 2015-02-05 | Board Of Regents Of The University Of Nebraska | Compositions and methods for the treatment of biofilm infections |
| EP3137454A1 (en) | 2014-04-28 | 2017-03-08 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine d1 ligands |
| KR101756934B1 (ko) | 2014-07-08 | 2017-07-12 | 연세대학교 산학협력단 | 피롤로[1,2-a]피라진 유도체, 이의 약학적으로 허용가능한 염, 이들 화합물의 제조방법 및 이를 유효성분으로 함유하는 골다공증 치료 또는 예방용 약학조성물 |
| ES2970715T3 (es) | 2016-12-22 | 2024-05-30 | Prec Pharmaceuticals Inc | Composiciones y métodos para inhibir la actividad de la arginasa |
| CR20230030A (es) | 2018-02-27 | 2023-03-10 | Incyte Corp | Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b (divisional 2020-0441) |
| MX2020012376A (es) | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
| MX2021000116A (es) | 2018-07-05 | 2021-03-29 | Incyte Corp | Derivados de pirazina fusionados como inhibidores de a2a/a2b. |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| TW202202498A (zh) * | 2020-07-01 | 2022-01-16 | 大陸商四川海思科製藥有限公司 | 一種並環雜環衍生物及其在醫藥上的應用 |
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| JP5227032B2 (ja) * | 2005-02-03 | 2013-07-03 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼの阻害剤として有用なピロロピリミジン |
| JP4652906B2 (ja) * | 2005-06-30 | 2011-03-16 | 富士夫 宮脇 | 振動型マイクロインジェクション装置 |
| CA2636701C (en) * | 2006-01-27 | 2014-08-05 | Shanghai Hengrui Pharmaceutical Co. Ltd. | Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors |
| WO2008057994A2 (en) * | 2006-11-03 | 2008-05-15 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| WO2008118823A2 (en) | 2007-03-26 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| GB0719803D0 (en) | 2007-10-10 | 2007-11-21 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| KR20100132550A (ko) | 2008-04-16 | 2010-12-17 | 포톨라 파마슈티컬스, 인코포레이티드 | ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드 |
| PE20110063A1 (es) | 2008-06-20 | 2011-02-16 | Genentech Inc | DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK |
| KR20110033223A (ko) | 2008-06-20 | 2011-03-30 | 제넨테크, 인크. | 트리아졸로피리딘 ｊａｋ 억제제 화합물 및 방법 |
| WO2010010184A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors |
| WO2010010188A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | Novel compounds useful for the treatment of degenerative and inflammatory diseases. |
| WO2010010189A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | Novel compounds useful for the treatment of degenerative and inflammatory diseases |
| 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 |
| CN102459258B (zh) * | 2009-06-05 | 2015-11-25 | 赛福伦公司 | 1,2,4-三唑并[1,5a]吡啶衍生物的制备和用途 |
| WO2011086098A1 (en) * | 2010-01-15 | 2011-07-21 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted bicyclic triazole derivatives as gamma secretase modulators |
| US20110190269A1 (en) | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
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| EP2609098A1 (en) | 2013-07-03 |
| JP5951610B2 (ja) | 2016-07-13 |
| WO2012025186A1 (en) | 2012-03-01 |
| US9023851B2 (en) | 2015-05-05 |
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| CN103068828B (zh) | 2015-09-09 |
| MX2013002198A (es) | 2013-03-18 |
| AR082726A1 (es) | 2012-12-26 |
| US20130225568A1 (en) | 2013-08-29 |
| AU2011295440A1 (en) | 2013-04-11 |
| CA2809331C (en) | 2018-09-25 |
| CA2809331A1 (en) | 2012-03-01 |
| CN103068828A (zh) | 2013-04-24 |
| EA201300282A1 (ru) | 2013-08-30 |
| SG188296A1 (en) | 2013-04-30 |
| KR20130110163A (ko) | 2013-10-08 |
| EP2609098B1 (en) | 2016-07-13 |
| ES2614128T3 (es) | 2017-05-29 |
| BR112013004517A2 (pt) | 2016-06-07 |
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