CN102015691B - 作为活化素样受体激酶(alk4或alk5)抑制剂的咪唑并吡啶衍生物 - Google Patents
作为活化素样受体激酶(alk4或alk5)抑制剂的咪唑并吡啶衍生物 Download PDFInfo
- Publication number
- CN102015691B CN102015691B CN200980115503.0A CN200980115503A CN102015691B CN 102015691 B CN102015691 B CN 102015691B CN 200980115503 A CN200980115503 A CN 200980115503A CN 102015691 B CN102015691 B CN 102015691B
- Authority
- CN
- China
- Prior art keywords
- pyridine
- pyridin
- imidazo
- base
- compound
- 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.)
- Expired - Fee Related
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/16—Central respiratory analeptics
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
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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
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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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
-
- 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
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Virology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Biotechnology (AREA)
- Gastroenterology & Hepatology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08155405 | 2008-04-29 | ||
| EP08155405.7 | 2008-04-29 | ||
| PCT/EP2009/055066 WO2009133070A1 (en) | 2008-04-29 | 2009-04-27 | Imidazo-pyridine derivatives as activin-like receptor kinase (alk4 or alk5) inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102015691A CN102015691A (zh) | 2011-04-13 |
| CN102015691B true CN102015691B (zh) | 2014-01-08 |
Family
ID=40043988
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200980115503.0A Expired - Fee Related CN102015691B (zh) | 2008-04-29 | 2009-04-27 | 作为活化素样受体激酶(alk4或alk5)抑制剂的咪唑并吡啶衍生物 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9079897B2 (https=) |
| EP (1) | EP2307402B1 (https=) |
| JP (1) | JP5507543B2 (https=) |
| KR (1) | KR20100130226A (https=) |
| CN (1) | CN102015691B (https=) |
| AU (1) | AU2009242145B2 (https=) |
| BR (1) | BRPI0911490A2 (https=) |
| CA (1) | CA2722131A1 (https=) |
| EA (1) | EA201001687A1 (https=) |
| ES (1) | ES2399175T3 (https=) |
| MX (1) | MX2010011867A (https=) |
| PL (1) | PL2307402T3 (https=) |
| PT (1) | PT2307402E (https=) |
| WO (1) | WO2009133070A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112012018954A2 (pt) | 2010-02-05 | 2016-04-12 | Merck Patent Gmbh | derivados de hetaril-[1,8]naftiridina |
| SG183233A1 (en) | 2010-02-22 | 2012-09-27 | Merck Patent Gmbh | Hetarylaminonaphthyridines |
| US9073918B2 (en) | 2010-05-20 | 2015-07-07 | Takeda Pharmaceutical Company Limited | Pyrazolo[4,3-b]pyridine-7-amine inhibitors of ALK5 |
| US8871744B2 (en) | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
| WO2012064043A2 (ko) | 2010-11-08 | 2012-05-18 | 에스케이케미칼 주식회사 | 폴리유산 수지, 이의 제조 방법 및 이를 포함하는 포장용 필름 |
| AU2012240656A1 (en) * | 2011-04-05 | 2013-10-24 | Academisch Ziekenhuis Leiden H.O.D.N. Lumc | Compounds and methods for altering activin receptor-like kinase signalling |
| JP2016510764A (ja) | 2013-03-07 | 2016-04-11 | カリフィア バイオ, インク.Califia Bio, Inc. | 混合系キナーゼ阻害剤および治療法 |
| US10179777B2 (en) | 2015-04-16 | 2019-01-15 | Merck Patent Gmbh | 3-(1H-benzimidazol-2-yl)-1H-pyridin-2-one derivatives |
| US10508082B2 (en) * | 2015-09-23 | 2019-12-17 | Dana-Farber Cancer Institute, Inc. | Substituted 6,11-dihydro-5H-benzo[b]carbazoles as inhibitors of ALK and SRPK |
| RU2642456C2 (ru) * | 2016-06-29 | 2018-01-25 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Ярославский государственный университет им. П.Г. Демидова" | Способ получения N-арилзамещенных 3H-имидазо[4,5-b]пиридинов |
| JP7007359B2 (ja) | 2016-07-29 | 2022-01-24 | シャンハイ インリ ファーマシューティカル カンパニー リミティド | 窒素含有芳香族複素環式化合物、その製造方法、薬物組成物および使用 |
| CN106831770A (zh) * | 2017-03-13 | 2017-06-13 | 牡丹江医学院 | 一种药物组合物及其用于治疗肝硬化的用途 |
| CN110066277B (zh) | 2018-01-24 | 2021-07-23 | 上海璎黎药业有限公司 | 芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用 |
| CN110066276B (zh) | 2018-01-24 | 2020-09-18 | 上海璎黎药业有限公司 | 芳香杂环化合物、其中间体、制备方法、药物组合物和应用 |
| US20200247812A1 (en) * | 2018-07-10 | 2020-08-06 | Integral Biosciences Private Limited | Heterocyclic compounds and methods of use |
| MX2021003904A (es) * | 2018-10-05 | 2021-10-26 | Annapurna Bio Inc | Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor apj. |
| JP2023509760A (ja) | 2020-01-08 | 2023-03-09 | シンシス セラピューティクス,インコーポレイテッド | Alk5阻害剤複合体およびその使用 |
| US20230174620A1 (en) | 2020-04-28 | 2023-06-08 | Acceleron Pharma Inc. | Actrii proteins and use in treating post-capillary pulmonary hypertension |
| EP4182308B1 (en) | 2020-07-15 | 2024-09-04 | Chiesi Farmaceutici S.p.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| EP4182323B1 (en) | 2020-07-15 | 2024-04-24 | Chiesi Farmaceutici S.p.A. | Pyrido oxazine amino derivatives as alk5 inhibitors |
| ES2982017T3 (es) | 2020-07-15 | 2024-10-14 | Chiesi Farm Spa | Derivados de pirido-oxazina como inhibidores de ALK5 |
| EP4267584A1 (en) | 2020-12-23 | 2023-11-01 | Chiesi Farmaceutici S.p.A. | Pyrido oxazine derivatives as alk5 inhibitors |
| US20250011299A1 (en) | 2021-09-21 | 2025-01-09 | Chiesi Farmaceutici S.P.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| EP4514802A1 (en) | 2022-04-27 | 2025-03-05 | Chiesi Farmaceutici S.p.A. | Imidazole derivatives as alk5 inhibitors |
| CN121712526A (zh) | 2023-06-13 | 2026-03-20 | 辛瑟斯治疗股份有限公司 | 抗cd5抗体及其用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0563001A1 (en) * | 1992-03-26 | 1993-09-29 | Neurosearch A/S | Imidazole compounds, their preparation and use |
| WO2001018000A1 (en) * | 1999-09-07 | 2001-03-15 | Merck Sharp & Dohme Limited | Imidazo-pyridine derivatives as ligands for gaba receptors |
| WO2004013138A2 (en) * | 2002-07-31 | 2004-02-12 | Smithkline Beecham Corporation | Imidazo`1,2-a!pyridines |
| WO2008006583A1 (en) * | 2006-07-14 | 2008-01-17 | Novartis Ag | Pyrimidine derivatives as alk-5 inhibitors |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005023246A1 (en) * | 2003-09-04 | 2005-03-17 | Aventis Pharmaceuticals Inc. | Substituted indoles as inhibitors of poly (adp-ribose) polymerase (parp) |
| CN101052640B (zh) * | 2004-09-03 | 2011-05-11 | 默克雪兰诺有限公司 | 吡啶亚甲基唑烷酮类及其作为磷酸肌醇抑制剂的用途 |
| JP2010508315A (ja) * | 2006-10-30 | 2010-03-18 | ノバルティス アーゲー | 抗炎症剤としてのヘテロ環式化合物 |
-
2009
- 2009-04-27 PT PT97381149T patent/PT2307402E/pt unknown
- 2009-04-27 WO PCT/EP2009/055066 patent/WO2009133070A1/en not_active Ceased
- 2009-04-27 CN CN200980115503.0A patent/CN102015691B/zh not_active Expired - Fee Related
- 2009-04-27 ES ES09738114T patent/ES2399175T3/es active Active
- 2009-04-27 MX MX2010011867A patent/MX2010011867A/es active IP Right Grant
- 2009-04-27 CA CA2722131A patent/CA2722131A1/en not_active Abandoned
- 2009-04-27 PL PL09738114T patent/PL2307402T3/pl unknown
- 2009-04-27 KR KR1020107024212A patent/KR20100130226A/ko not_active Ceased
- 2009-04-27 EP EP09738114A patent/EP2307402B1/en not_active Not-in-force
- 2009-04-27 BR BRPI0911490A patent/BRPI0911490A2/pt not_active IP Right Cessation
- 2009-04-27 EA EA201001687A patent/EA201001687A1/ru unknown
- 2009-04-27 JP JP2011506677A patent/JP5507543B2/ja not_active Expired - Fee Related
- 2009-04-27 US US12/935,405 patent/US9079897B2/en not_active Expired - Fee Related
- 2009-04-27 AU AU2009242145A patent/AU2009242145B2/en not_active Ceased
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0563001A1 (en) * | 1992-03-26 | 1993-09-29 | Neurosearch A/S | Imidazole compounds, their preparation and use |
| WO2001018000A1 (en) * | 1999-09-07 | 2001-03-15 | Merck Sharp & Dohme Limited | Imidazo-pyridine derivatives as ligands for gaba receptors |
| WO2004013138A2 (en) * | 2002-07-31 | 2004-02-12 | Smithkline Beecham Corporation | Imidazo`1,2-a!pyridines |
| WO2008006583A1 (en) * | 2006-07-14 | 2008-01-17 | Novartis Ag | Pyrimidine derivatives as alk-5 inhibitors |
Non-Patent Citations (2)
| Title |
|---|
| A concise synthesis of quinazolinone TGF-b RI inhibitor through one-pot three-component Suzuki–Miyaura/etherification and imidate–amide rearrangement reactions;Hong-yu Li, et al.;《Tetrahedron》;20070826;第63卷;第11763-11770页 * |
| Synthesis and biological evaluation of novel 2,4,5-triaryl-1H-pyrazol-3(2H)-ones as inhibitors of ALK5;Xing Zhou Li, et al.;《Chinses Chemical letters 》;20081231;第19卷;第379-382页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2011518856A (ja) | 2011-06-30 |
| US20110060004A1 (en) | 2011-03-10 |
| JP5507543B2 (ja) | 2014-05-28 |
| CA2722131A1 (en) | 2009-11-05 |
| KR20100130226A (ko) | 2010-12-10 |
| AU2009242145A1 (en) | 2009-11-05 |
| PT2307402E (pt) | 2013-02-15 |
| ES2399175T3 (es) | 2013-03-26 |
| MX2010011867A (es) | 2010-11-26 |
| US9079897B2 (en) | 2015-07-14 |
| EP2307402B1 (en) | 2012-11-07 |
| BRPI0911490A2 (pt) | 2016-01-05 |
| CN102015691A (zh) | 2011-04-13 |
| EA201001687A1 (ru) | 2011-06-30 |
| WO2009133070A1 (en) | 2009-11-05 |
| AU2009242145B2 (en) | 2012-07-05 |
| EP2307402A1 (en) | 2011-04-13 |
| PL2307402T3 (pl) | 2013-05-31 |
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