JP5677425B2 - Pi3k阻害剤としてのピリミジノン - Google Patents
Pi3k阻害剤としてのピリミジノン Download PDFInfo
- Publication number
- JP5677425B2 JP5677425B2 JP2012518563A JP2012518563A JP5677425B2 JP 5677425 B2 JP5677425 B2 JP 5677425B2 JP 2012518563 A JP2012518563 A JP 2012518563A JP 2012518563 A JP2012518563 A JP 2012518563A JP 5677425 B2 JP5677425 B2 JP 5677425B2
- Authority
- JP
- Japan
- Prior art keywords
- thiazolo
- methyl
- pyrimidin
- ethyl
- purin
- 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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- 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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- 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
- C07D471/12—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 three hetero rings
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
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- A61P11/16—Central respiratory analeptics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- 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
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- A61P9/00—Drugs for disorders of the cardiovascular system
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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
- A61P9/10—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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- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22116009P | 2009-06-29 | 2009-06-29 | |
| US61/221,160 | 2009-06-29 | ||
| US25976509P | 2009-11-10 | 2009-11-10 | |
| US61/259,765 | 2009-11-10 | ||
| PCT/US2010/040150 WO2011008487A1 (en) | 2009-06-29 | 2010-06-28 | Pyrimidinones as pi3k inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014223540A Division JP2015042673A (ja) | 2009-06-29 | 2014-10-31 | Pi3k阻害剤としてのピリミジノン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012532131A JP2012532131A (ja) | 2012-12-13 |
| JP2012532131A5 JP2012532131A5 (enExample) | 2013-08-15 |
| JP5677425B2 true JP5677425B2 (ja) | 2015-02-25 |
Family
ID=42575792
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012518563A Expired - Fee Related JP5677425B2 (ja) | 2009-06-29 | 2010-06-28 | Pi3k阻害剤としてのピリミジノン |
| JP2014223540A Pending JP2015042673A (ja) | 2009-06-29 | 2014-10-31 | Pi3k阻害剤としてのピリミジノン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014223540A Pending JP2015042673A (ja) | 2009-06-29 | 2014-10-31 | Pi3k阻害剤としてのピリミジノン |
Country Status (33)
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8754089B2 (en) * | 2009-06-25 | 2014-06-17 | Amgen Inc. | Heterocyclic compounds and their uses |
| PE20120493A1 (es) | 2009-06-29 | 2012-05-20 | Incyte Corp | Pirimidinonas como inhibidores de pi3k |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| TW201130842A (en) * | 2009-12-18 | 2011-09-16 | Incyte Corp | Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors |
| AR081823A1 (es) | 2010-04-14 | 2012-10-24 | Incyte Corp | DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| JP2013544832A (ja) | 2010-12-03 | 2013-12-19 | アラーガン インコーポレイテッド | スフィンゴシン−1−リン酸(s1p)受容体モジュレーターとしての新規オキサジアゾール誘導体 |
| ES2764848T3 (es) | 2010-12-20 | 2020-06-04 | Incyte Holdings Corp | N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K |
| WO2012125629A1 (en) * | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| KR20230038593A (ko) | 2011-09-02 | 2023-03-20 | 인사이트 홀딩스 코포레이션 | Pi3k 억제제로서 헤테로시클릴아민 |
| PL2790705T3 (pl) | 2011-12-15 | 2018-06-29 | Novartis Ag | Zastosowanie inhibitorów czynności lub funkcji PI3K |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| TW201414734A (zh) | 2012-07-10 | 2014-04-16 | Takeda Pharmaceutical | 氮雜吲哚衍生物 |
| WO2014015523A1 (en) | 2012-07-27 | 2014-01-30 | Hutchison Medipharma Limited | Novel heteroaryl and heterocycle compounds, compositions and methods |
| JP6434416B2 (ja) | 2012-11-08 | 2018-12-05 | ライゼン・ファーマシューティカルズ・エスアー | PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物 |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| HUE050215T2 (hu) | 2013-01-15 | 2020-11-30 | Incyte Holdings Corp | Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek |
| TWI841376B (zh) | 2013-03-01 | 2024-05-01 | 美商英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途 |
| TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作pim激酶抑制劑之呋喃并-及噻吩并-吡啶甲醯胺化合物 |
| WO2015091532A1 (en) * | 2013-12-19 | 2015-06-25 | Almirall, S.A. | Pyrrolopyrimidine derivatives as pi3k inhibitors |
| WO2015106014A1 (en) | 2014-01-09 | 2015-07-16 | Takeda Pharmaceutical Company Limited | Azaindole derivatives |
| UY35945A (es) | 2014-01-09 | 2015-08-31 | Takeda Pharmaceutical | Derivados de azaindol |
| MA39984B1 (fr) * | 2014-04-08 | 2020-12-31 | Incyte Corp | Traitement d'affections malignes par lymphocytes b par un inhibiteur jak et pi3k combiné |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| EP3159342B1 (en) * | 2014-06-17 | 2020-08-05 | Cisen Pharmaceutical Co., Ltd. | Pyridino[1,2-a]pyrimidone analogue used as mtor/pi3k inhibitor |
| KR20170082490A (ko) * | 2014-07-04 | 2017-07-14 | 루핀 리미티드 | Pi3k 억제제로서 퀴놀리지논 유도체 |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
| AU2015341186B2 (en) | 2014-11-01 | 2019-11-14 | Fochon Biosciences, Ltd. | Certain protein kinase inhibitors |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| WO2016130501A1 (en) | 2015-02-09 | 2016-08-18 | Incyte Corporation | Aza-heteroaryl compounds as pi3k-gamma inhibitors |
| PH12017501538B1 (en) | 2015-02-27 | 2024-02-14 | Incyte Holdings Corp | Salts of p13k inhibitor and processes for their preparation |
| CN106008479B (zh) * | 2015-03-06 | 2020-01-10 | 南京圣和药业股份有限公司 | 作为磷脂酰肌醇3-激酶δ抑制剂的取代嘧啶类化合物及其应用 |
| US9840503B2 (en) | 2015-05-11 | 2017-12-12 | Incyte Corporation | Heterocyclic compounds and uses thereof |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| US20160362424A1 (en) * | 2015-05-11 | 2016-12-15 | Incyte Corporation | Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| US9708333B2 (en) | 2015-08-12 | 2017-07-18 | Incyte Corporation | Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors |
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| SI3371190T1 (sl) | 2015-11-06 | 2022-08-31 | Incyte Corporation | Heterociklične spojine kot inhibitorji PI3K gama |
| TWI713655B (zh) * | 2015-12-16 | 2020-12-21 | 大陸商上海嘉坦醫藥科技有限公司 | 吡啶並[1,2-a]嘧啶酮類似物的晶型及其製備方法和中間體 |
| WO2017103825A1 (en) | 2015-12-18 | 2017-06-22 | Lupin Limited | Quinolizinone derivatives as pi3k inhibitors |
| WO2017120194A1 (en) | 2016-01-05 | 2017-07-13 | Incyte Corporation | Pyridine and pyridimine compounds as pi3k-gamma inhibitors |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| PT3436461T (pt) | 2016-03-28 | 2024-01-23 | Incyte Corp | Compostos de pirrolotriazina como inibidores de tam |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2017223414A1 (en) | 2016-06-24 | 2017-12-28 | Incyte Corporation | HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS |
| US10633387B2 (en) | 2017-09-27 | 2020-04-28 | Incyte Corporation | Salts of TAM inhibitors |
| SI3697789T1 (sl) | 2017-10-18 | 2022-04-29 | Incyte Corporation | Kondenzirani imidazolni derivati, substituirani s terciarnimi hidroksi skupinami, kot zaviralci PI3K-gama |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| CN112469418A (zh) | 2018-06-01 | 2021-03-09 | 因赛特公司 | 治疗pi3k相关病症的给药方案 |
| SI3813800T1 (sl) | 2018-06-29 | 2025-07-31 | Incyte Corporation | Formulacije zaviralca axl/mer |
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