CN101883774A - 噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途 - Google Patents
噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途 Download PDFInfo
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- CN101883774A CN101883774A CN2008801190434A CN200880119043A CN101883774A CN 101883774 A CN101883774 A CN 101883774A CN 2008801190434 A CN2008801190434 A CN 2008801190434A CN 200880119043 A CN200880119043 A CN 200880119043A CN 101883774 A CN101883774 A CN 101883774A
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- phenyl
- oxa
- pyrimidine
- azabicyclo
- pyrazolo
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98033207P | 2007-10-16 | 2007-10-16 | |
| US60/980,332 | 2007-10-16 | ||
| US2759508P | 2008-02-11 | 2008-02-11 | |
| US61/027,595 | 2008-02-11 | ||
| PCT/US2008/079940 WO2009052145A1 (en) | 2007-10-16 | 2008-10-15 | Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101883774A true CN101883774A (zh) | 2010-11-10 |
Family
ID=40345078
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008801190434A Pending CN101883774A (zh) | 2007-10-16 | 2008-10-15 | 噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8129371B2 (enExample) |
| EP (1) | EP2212333A1 (enExample) |
| JP (1) | JP2011500702A (enExample) |
| KR (1) | KR20100083170A (enExample) |
| CN (1) | CN101883774A (enExample) |
| AP (1) | AP2010005234A0 (enExample) |
| AR (1) | AR068898A1 (enExample) |
| AU (1) | AU2008312631A1 (enExample) |
| BR (1) | BRPI0817681A2 (enExample) |
| CA (1) | CA2702838A1 (enExample) |
| CL (1) | CL2008003061A1 (enExample) |
| CO (1) | CO6321257A2 (enExample) |
| CR (1) | CR11373A (enExample) |
| DO (1) | DOP2010000118A (enExample) |
| EA (1) | EA201000484A1 (enExample) |
| EC (1) | ECSP10010112A (enExample) |
| IL (1) | IL205109A0 (enExample) |
| MA (1) | MA31884B1 (enExample) |
| MX (1) | MX2010004260A (enExample) |
| NI (1) | NI201000060A (enExample) |
| PA (1) | PA8799101A1 (enExample) |
| PE (1) | PE20091384A1 (enExample) |
| TN (1) | TN2010000171A1 (enExample) |
| TW (1) | TW200922593A (enExample) |
| WO (1) | WO2009052145A1 (enExample) |
| ZA (1) | ZA201003430B (enExample) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013152717A1 (zh) * | 2012-04-10 | 2013-10-17 | 上海昀怡健康管理咨询有限公司 | 稠合嘧啶类化合物,其制备方法,中间体,组合物和应用 |
| CN104080789A (zh) * | 2012-01-31 | 2014-10-01 | 南京奥昭生物科技有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
| CN108358949A (zh) * | 2018-03-01 | 2018-08-03 | 南京法恩化学有限公司 | 一种2,4-二氯噻吩并[3,2-d]嘧啶的制备方法 |
| CN109824701A (zh) * | 2019-03-26 | 2019-05-31 | 武汉工程大学 | 一种吡啶并噻唑类化合物及其制备方法和应用 |
| CN110850012A (zh) * | 2018-08-21 | 2020-02-28 | 成都弘达药业有限公司 | 一种1-(2,3-二氯苯基)哌嗪盐酸盐及其有关物质的检测方法 |
| CN111646995A (zh) * | 2019-03-04 | 2020-09-11 | 四川大学 | 4-氨基-嘧啶并氮杂环-苯基脲类衍生物及其制备方法和用途 |
| CN113278015A (zh) * | 2021-05-31 | 2021-08-20 | 云南大学 | 一种荧光探针及其制备方法和应用 |
| WO2025201469A1 (zh) * | 2024-03-28 | 2025-10-02 | 励缔(杭州)医药科技有限公司 | 具有mTOR抑制活性的有机化合物及其用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1679668B1 (en) * | 1996-09-04 | 2010-01-27 | Intertrust Technologies Corp. | Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management |
| US20030133939A1 (en) | 2001-01-17 | 2003-07-17 | Genecraft, Inc. | Binding domain-immunoglobulin fusion proteins |
| US7754208B2 (en) | 2001-01-17 | 2010-07-13 | Trubion Pharmaceuticals, Inc. | Binding domain-immunoglobulin fusion proteins |
| PT1912675E (pt) | 2005-07-25 | 2014-05-09 | Emergent Product Dev Seattle | Moléculas de ligaçao especificas para cd37 e especificas para cd20 |
| MX380352B (es) | 2006-06-12 | 2025-03-12 | Aptevo Res & Development Llc | Proteinas de union multivalentes monocatenarias con funcion efectora. |
| US7820665B2 (en) | 2007-12-19 | 2010-10-26 | Amgen Inc. | Imidazopyridazine inhibitors of PI3 kinase for cancer treatment |
| RS51975B (sr) | 2008-04-11 | 2012-02-29 | Emergent Product Development Seattle Llc. | Cd37 imunoterapeutski proizvod i njegova kombinacija sa bifunkcionalnim hemoterapeutskim sredstvom |
| TW201004963A (en) * | 2008-07-03 | 2010-02-01 | Targacept Inc | Derivatives of oxabispidine as neuronal nicotinic acetylcholine receptor ligands |
| PE20110403A1 (es) * | 2008-07-31 | 2011-07-04 | Genentech Inc | Compuestos biciclicos fusionados de pirimidina en el tratamiento del cancer |
| RS53350B (sr) | 2008-09-22 | 2014-10-31 | Array Biopharma, Inc. | Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze |
| TWI378933B (en) | 2008-10-14 | 2012-12-11 | Daiichi Sankyo Co Ltd | Morpholinopurine derivatives |
| PT2725028T (pt) | 2008-10-22 | 2016-08-31 | Array Biopharma Inc | Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk |
| DK2385832T3 (en) | 2009-01-08 | 2015-09-21 | Curis Inc | Phosphoinositid-3-kinase-inhibitorer med en zink-bindingsdel |
| JP5649643B2 (ja) * | 2009-04-17 | 2015-01-07 | ワイス・エルエルシー | ピリミジン化合物、mTORキナーゼおよびPI3キナーゼ阻害剤としてのそれらの使用、ならびにそれらの合成 |
| AU2010254161A1 (en) * | 2009-05-27 | 2011-11-10 | F. Hoffmann-La Roche Ag | Bicyclic pyrimidine PI3K inhibitor compounds selective for p110 delta, and methods of use |
| US20100331305A1 (en) * | 2009-06-24 | 2010-12-30 | Genentech, Inc. | Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| US20110021515A1 (en) * | 2009-07-24 | 2011-01-27 | Takeda Pharmaceutical Company Limited | Dihyrofuropyrmindine compounds |
| KR101147550B1 (ko) | 2009-10-22 | 2012-05-17 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-d]피리미딘 화합물 |
| KR101447789B1 (ko) * | 2009-11-12 | 2014-10-06 | 에프. 호프만-라 로슈 아게 | N-7 치환된 퓨린 및 피라졸로피리미딘 화합물, 조성물 및 사용 방법 |
| RU2607635C2 (ru) * | 2009-11-12 | 2017-01-10 | Ф.Хоффманн-Ля Рош Аг | N-9-замещенные пуриновые соединения, композиции и способы применения |
| WO2011078795A1 (en) * | 2009-12-21 | 2011-06-30 | S*Bio Pte Ltd | Bridged morpholino substituted purines |
| EP2525659B1 (en) | 2010-01-19 | 2019-02-27 | Merck Sharp & Dohme Corp. | PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS |
| EP2992878A1 (en) | 2010-02-03 | 2016-03-09 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| JP2013523807A (ja) | 2010-04-05 | 2013-06-17 | ワイス・エルエルシー | Pi3kにより誘発される癌のためのバイオマーカー |
| HUE044025T2 (hu) | 2010-05-20 | 2019-09-30 | Array Biopharma Inc | Makrociklusos vegyületek mint TRK-kináz inhibitorok |
| ES2986590T3 (es) | 2010-06-14 | 2024-11-12 | Scripps Research Inst | Reprogramación de células hacia un nuevo destino |
| WO2012071519A1 (en) * | 2010-11-24 | 2012-05-31 | Exelixis, Inc. | Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| WO2012099581A1 (en) | 2011-01-19 | 2012-07-26 | Takeda Pharmaceutical Company Limited | Dihydrofuropyrimidine compounds |
| AU2012290056B2 (en) | 2011-08-03 | 2015-03-19 | Signal Pharmaceuticals, Llc | Identification of gene expression profile as a predictive biomarker for LKB1 status |
| FR2985257B1 (fr) * | 2011-12-28 | 2014-02-14 | Sanofi Sa | Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique |
| CN103374021B (zh) * | 2012-04-21 | 2015-10-28 | 通化济达医药有限公司 | 含有锌结合基的吡啶并嘧啶类HDAC和mTOR抑制剂 |
| JP6301316B2 (ja) | 2012-05-23 | 2018-03-28 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 内胚葉細胞および肝実質細胞の組成物ならびにそれらの細胞を入手および使用する方法 |
| CN103450204B (zh) * | 2012-05-31 | 2016-08-17 | 中国科学院上海药物研究所 | 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途 |
| UA125503C2 (uk) | 2012-06-13 | 2022-04-13 | Інсайт Холдинґс Корпорейшн | Заміщені трициклічні сполуки як інгібітори fgfr |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| TWI654979B (zh) | 2013-04-17 | 2019-04-01 | 美商標誌製藥公司 | 使用tor激酶抑制劑組合療法以治療癌症之方法 |
| WO2014172431A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| CA2909579A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
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| JP6382945B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ,エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| WO2014172432A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| KR102459285B1 (ko) | 2013-04-17 | 2022-10-27 | 시그날 파마소티칼 엘엘씨 | 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법 |
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| FR3015483B1 (fr) * | 2013-12-23 | 2016-01-01 | Servier Lab | Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
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| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | Signal Pharmaceuticals, LLC | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| CR20160525A (es) | 2014-05-14 | 2016-12-20 | Pfizer | Pirazolopiridinas y pirazolopirimidinas |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| FI3699181T3 (fi) | 2014-11-16 | 2023-03-28 | Array Biopharma Inc | Kiteinen muoto (s)-n-(5-((r)-2-(2,5-diluorifenyyli)-pyrrolidin-1-yyli)-pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidivetyysulfaatista |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| BR112018005573A2 (pt) | 2015-09-21 | 2019-01-22 | Aptevo Research And Development Llc | ?polipeptídeos de ligação a cd3? |
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Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3649395B2 (ja) | 2000-04-27 | 2005-05-18 | 山之内製薬株式会社 | 縮合ヘテロアリール誘導体 |
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- 2008-10-15 US US12/251,712 patent/US8129371B2/en not_active Expired - Fee Related
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- 2010-04-16 EC EC2010010112A patent/ECSP10010112A/es unknown
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- 2010-04-16 TN TN2010000171A patent/TN2010000171A1/fr unknown
- 2010-04-20 CO CO10046199A patent/CO6321257A2/es not_active Application Discontinuation
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Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN104080789A (zh) * | 2012-01-31 | 2014-10-01 | 南京奥昭生物科技有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
| CN104080789B (zh) * | 2012-01-31 | 2016-05-11 | 南京奥昭生物科技有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
| WO2013152717A1 (zh) * | 2012-04-10 | 2013-10-17 | 上海昀怡健康管理咨询有限公司 | 稠合嘧啶类化合物,其制备方法,中间体,组合物和应用 |
| US9499561B2 (en) | 2012-04-10 | 2016-11-22 | Shanghai Yingli Pharmaceutical Co., Ltd. | Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof |
| CN108358949A (zh) * | 2018-03-01 | 2018-08-03 | 南京法恩化学有限公司 | 一种2,4-二氯噻吩并[3,2-d]嘧啶的制备方法 |
| CN110850012A (zh) * | 2018-08-21 | 2020-02-28 | 成都弘达药业有限公司 | 一种1-(2,3-二氯苯基)哌嗪盐酸盐及其有关物质的检测方法 |
| CN111646995A (zh) * | 2019-03-04 | 2020-09-11 | 四川大学 | 4-氨基-嘧啶并氮杂环-苯基脲类衍生物及其制备方法和用途 |
| CN111646995B (zh) * | 2019-03-04 | 2023-03-21 | 四川大学 | 4-氨基-嘧啶并氮杂环-苯基脲类衍生物及其制备方法和用途 |
| CN109824701A (zh) * | 2019-03-26 | 2019-05-31 | 武汉工程大学 | 一种吡啶并噻唑类化合物及其制备方法和应用 |
| CN109824701B (zh) * | 2019-03-26 | 2021-08-13 | 武汉工程大学 | 一种吡啶并噻唑类化合物及其制备方法和应用 |
| CN113278015A (zh) * | 2021-05-31 | 2021-08-20 | 云南大学 | 一种荧光探针及其制备方法和应用 |
| WO2025201469A1 (zh) * | 2024-03-28 | 2025-10-02 | 励缔(杭州)医药科技有限公司 | 具有mTOR抑制活性的有机化合物及其用途 |
Also Published As
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|---|---|
| EA201000484A1 (ru) | 2010-12-30 |
| CR11373A (es) | 2010-05-03 |
| AP2010005234A0 (en) | 2010-04-30 |
| AR068898A1 (es) | 2009-12-16 |
| BRPI0817681A2 (pt) | 2015-04-14 |
| IL205109A0 (en) | 2010-11-30 |
| WO2009052145A1 (en) | 2009-04-23 |
| JP2011500702A (ja) | 2011-01-06 |
| KR20100083170A (ko) | 2010-07-21 |
| CO6321257A2 (es) | 2011-09-20 |
| ZA201003430B (en) | 2011-02-23 |
| US8129371B2 (en) | 2012-03-06 |
| MX2010004260A (es) | 2010-04-30 |
| ECSP10010112A (es) | 2010-08-31 |
| CL2008003061A1 (es) | 2009-01-09 |
| AU2008312631A1 (en) | 2009-04-23 |
| TN2010000171A1 (fr) | 2011-11-11 |
| NI201000060A (es) | 2010-10-04 |
| PE20091384A1 (es) | 2009-09-09 |
| TW200922593A (en) | 2009-06-01 |
| EP2212333A1 (en) | 2010-08-04 |
| DOP2010000118A (es) | 2010-06-30 |
| MA31884B1 (fr) | 2010-12-01 |
| US20090098086A1 (en) | 2009-04-16 |
| PA8799101A1 (es) | 2009-05-15 |
| CA2702838A1 (en) | 2009-04-23 |
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