CA2766100C - Pyrimidinones as pi3k inhibitors - Google Patents
Pyrimidinones as pi3k inhibitors Download PDFInfo
- Publication number
- CA2766100C CA2766100C CA2766100A CA2766100A CA2766100C CA 2766100 C CA2766100 C CA 2766100C CA 2766100 A CA2766100 A CA 2766100A CA 2766100 A CA2766100 A CA 2766100A CA 2766100 C CA2766100 C CA 2766100C
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- alkyl
- independently selected
- halo
- alkynyl
- alkenyl
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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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- 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
- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Hematology (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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2766100A1 CA2766100A1 (en) | 2011-01-20 |
| CA2766100C true CA2766100C (en) | 2018-05-22 |
Family
ID=42575792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2766100A Active CA2766100C (en) | 2009-06-29 | 2010-06-28 | Pyrimidinones as pi3k inhibitors |
Country Status (33)
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2445898A2 (en) * | 2009-06-25 | 2012-05-02 | Amgen, Inc | 4h-pyrido[1,2-a]pyrimidin-4-one derivatives as pi3k inhibitors |
| EP2845856A1 (en) | 2009-06-29 | 2015-03-11 | Incyte Corporation | Pyrimidinones as PI3K inhibitors |
| WO2011075630A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors |
| US8759359B2 (en) * | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| EP2558463A1 (en) | 2010-04-14 | 2013-02-20 | Incyte Corporation | Fused derivatives as i3 inhibitors |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| AU2011337083A1 (en) | 2010-12-03 | 2013-07-11 | Allergan, Inc. | Novel oxadiazole derivatives as sphingosine 1-phosphate (S1P) receptor modulators |
| TW201249844A (en) | 2010-12-20 | 2012-12-16 | Incyte Corp | N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors |
| WO2012125629A1 (en) * | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| UA121539C2 (uk) | 2011-09-02 | 2020-06-25 | Інсайт Холдинґс Корпорейшн | Гетероцикліламіни як інгібітори рі3к |
| JP6117235B2 (ja) | 2011-12-15 | 2017-04-19 | ノバルティス アーゲー | Pi3kの活性または機能の阻害剤の使用 |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| UY34893A (es) | 2012-07-10 | 2014-02-28 | Takeda Pharmaceutical | Derivados de azaindol |
| WO2014015523A1 (en) * | 2012-07-27 | 2014-01-30 | Hutchison Medipharma Limited | Novel heteroaryl and heterocycle compounds, compositions and methods |
| WO2014072937A1 (en) | 2012-11-08 | 2014-05-15 | Rhizen Pharmaceuticals Sa | Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
| 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 |
| AR099052A1 (es) | 2014-01-09 | 2016-06-29 | Takeda Pharmaceuticals Co | Derivados de azaindol |
| WO2015106014A1 (en) | 2014-01-09 | 2015-07-16 | Takeda Pharmaceutical Company Limited | Azaindole derivatives |
| CN106413716B (zh) * | 2014-04-08 | 2020-03-27 | 因赛特公司 | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| BR112016029825B1 (pt) * | 2014-06-17 | 2020-10-27 | Cisen Pharmaceutical Co., Ltd. | composto |
| SG11201610770PA (en) * | 2014-07-04 | 2017-01-27 | Lupin Ltd | Quinolizinone derivatives as pi3k inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic 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 |
| ES2879809T3 (es) * | 2014-11-01 | 2021-11-23 | Shanghai Fochon Pharmaceutical Co Ltd | Ciertos inhibidores de proteínas quinasas |
| 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 |
| UA122332C2 (uk) | 2015-02-27 | 2020-10-26 | Інсайт Корпорейшн | Солі інгібітора pi3k і способи їх отримання |
| 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 |
| WO2016183063A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Crystalline forms of a pi3k inhibitor |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | 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 |
| US9840503B2 (en) | 2015-05-11 | 2017-12-12 | Incyte Corporation | Heterocyclic compounds and uses thereof |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| WO2017027717A1 (en) | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
| US10053465B2 (en) | 2015-08-26 | 2018-08-21 | Incyte Corporation | Pyrrolopyrimidine derivatives as TAM inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| TWI744256B (zh) | 2015-11-06 | 2021-11-01 | 美商英塞特公司 | 作為PI3K-γ抑制劑之雜環化合物 |
| 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 |
| TW201734003A (zh) | 2016-01-05 | 2017-10-01 | 英塞特公司 | 作為PI3K-γ抑制劑之吡啶及嘧啶化合物 |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| CN114456176B (zh) * | 2016-03-28 | 2024-08-30 | 因赛特公司 | 作为tam抑制剂的吡咯并三嗪化合物 |
| US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| AR108875A1 (es) | 2016-06-24 | 2018-10-03 | Incyte Corp | COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g |
| KR102739325B1 (ko) | 2017-09-27 | 2024-12-09 | 인사이트 코포레이션 | Tam 억제제로서 유용한 피롤로트리아진 유도체의 염 |
| AU2018350980C1 (en) | 2017-10-18 | 2024-12-12 | Incyte Corporation | Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-y gamma inhibitors |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| MX2020012826A (es) | 2018-06-01 | 2021-03-09 | Incyte Corp | Regimen de dosificacion para el tratamiento de trastornos relacionados con fosfatidilinositol 3-cinasas (pi3k). |
| US11241438B2 (en) | 2018-06-29 | 2022-02-08 | Incyte Corporation | Formulations of an AXL/MER inhibitor |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| US11078204B2 (en) | 2018-11-13 | 2021-08-03 | Incyte Corporation | Heterocyclic derivatives as PI3K inhibitors |
| US11161838B2 (en) | 2018-11-13 | 2021-11-02 | Incyte Corporation | Heterocyclic derivatives as PI3K inhibitors |
| WO2020102216A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Substituted heterocyclic derivatives as pi3k inhibitors |
| CN110078747B (zh) * | 2019-04-11 | 2020-04-10 | 河南科技大学第一附属医院 | 一种用于医院消毒的新型噻唑类药物分子及其制备方法 |
| JP2021008453A (ja) | 2019-07-02 | 2021-01-28 | エフェクター・セラピューティクス,インコーポレーテッド | 翻訳阻害剤およびその使用 |
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| 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 |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| WO2016183063A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Crystalline forms of a pi3k inhibitor |
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