JP2013533884A5 - - Google Patents
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- Publication number
- JP2013533884A5 JP2013533884A5 JP2013518689A JP2013518689A JP2013533884A5 JP 2013533884 A5 JP2013533884 A5 JP 2013533884A5 JP 2013518689 A JP2013518689 A JP 2013518689A JP 2013518689 A JP2013518689 A JP 2013518689A JP 2013533884 A5 JP2013533884 A5 JP 2013533884A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- haloalkyl
- halo
- cyano
- substituted
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 103
- 125000005843 halogen group Chemical group 0.000 claims 20
- 125000004093 cyano group Chemical group *C#N 0.000 claims 16
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 8
- 229920006395 saturated elastomer Polymers 0.000 claims 7
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 230000002757 inflammatory effect Effects 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000000464 thioxo group Chemical group S=* 0.000 claims 2
- 206010027654 Allergic conditions Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 1
- 208000002552 acute disseminated encephalomyelitis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36101410P | 2010-07-02 | 2010-07-02 | |
| US61/361,014 | 2010-07-02 | ||
| PCT/US2011/042519 WO2012003271A1 (en) | 2010-07-02 | 2011-06-30 | Heterocyclic compounds and their use as inhibitors of pi3k activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013533884A JP2013533884A (ja) | 2013-08-29 |
| JP2013533884A5 true JP2013533884A5 (enExample) | 2014-08-14 |
Family
ID=44307237
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013518689A Withdrawn JP2013533884A (ja) | 2010-07-02 | 2011-06-30 | Pi3k活性阻害剤としての複素環化合物およびそれらの使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20130096134A1 (enExample) |
| EP (1) | EP2588469A1 (enExample) |
| JP (1) | JP2013533884A (enExample) |
| AU (1) | AU2011272850A1 (enExample) |
| CA (1) | CA2803624A1 (enExample) |
| MX (1) | MX2012015134A (enExample) |
| WO (1) | WO2012003271A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AR081823A1 (es) | 2010-04-14 | 2012-10-24 | Incyte Corp | DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd |
| JP5951600B2 (ja) | 2010-05-21 | 2016-07-13 | インフィニティー ファーマシューティカルズ, インコーポレイテッド | キナーゼ調節のための、化合物、組成物および方法 |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| JP2013541591A (ja) * | 2010-11-04 | 2013-11-14 | アムジエン・インコーポレーテツド | 複素環化合物およびそれらの使用 |
| 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 |
| US8785470B2 (en) | 2011-08-29 | 2014-07-22 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| KR20230038593A (ko) | 2011-09-02 | 2023-03-20 | 인사이트 홀딩스 코포레이션 | Pi3k 억제제로서 헤테로시클릴아민 |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| DK2834231T3 (en) * | 2012-04-04 | 2016-04-18 | Amgen Inc | HETEROCYCLIC COMPOUNDS AND THEIR USES |
| ES2652514T3 (es) | 2012-11-08 | 2018-02-02 | Pfizer Inc. | Compuestos heteroaromáticos como ligandos de dopamina D1 |
| 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 |
| EP2935246B1 (en) | 2012-12-21 | 2018-07-25 | Gilead Calistoga LLC | Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors |
| AU2013364068B2 (en) | 2012-12-21 | 2016-10-20 | Gilead Calistoga Llc | Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors |
| US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
| AR096621A1 (es) | 2013-06-14 | 2016-01-20 | Gilead Sciences Inc | Inhibidores de isómeros de la fosfatidilinositol 3-quinasa (pi3k) |
| CN104513235B (zh) * | 2013-09-02 | 2017-12-05 | 广东东阳光药业有限公司 | 取代的氨基嘧啶类化合物及其使用方法和用途 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| KR20170082490A (ko) | 2014-07-04 | 2017-07-14 | 루핀 리미티드 | Pi3k 억제제로서 퀴놀리지논 유도체 |
| BR112017003745A2 (pt) | 2014-08-29 | 2017-12-05 | Tes Pharma S R L | inibidores de semialdeído descarboxilase de ácido alfa-amino-beta-carboximucônico |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| PH12017501538B1 (en) | 2015-02-27 | 2024-02-14 | Incyte Holdings Corp | Salts of p13k inhibitor and processes for their preparation |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| US10442799B1 (en) | 2018-04-07 | 2019-10-15 | Fuqiang Ruan | Heterocyclic compounds and uses thereof |
| 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 |
| AU2022380979A1 (en) | 2021-11-02 | 2024-06-06 | Flare Therapeutics Inc. | Pparg inverse agonists and uses thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| US6043062A (en) | 1995-02-17 | 2000-03-28 | The Regents Of The University Of California | Constitutively active phosphatidylinositol 3-kinase and uses thereof |
| GB9611460D0 (en) | 1996-06-01 | 1996-08-07 | Ludwig Inst Cancer Res | Novel lipid kinase |
| US5858753A (en) | 1996-11-25 | 1999-01-12 | Icos Corporation | Lipid kinase |
| US5822910A (en) | 1997-10-02 | 1998-10-20 | Shewmake; I. W. | Fishing line tensioning device |
| PL2137186T3 (pl) | 2007-03-23 | 2016-09-30 | Związki heterocykliczne i ich zastosowania | |
| ES2587738T3 (es) * | 2007-12-21 | 2016-10-26 | Ucb Biopharma Sprl | Derivados de quinoxalina y quinolina como inhibidores de quinasa |
| CA2738429C (en) * | 2008-09-26 | 2016-10-25 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| ES2598358T3 (es) * | 2009-02-13 | 2017-01-27 | Ucb Pharma, S.A. | Derivados de quinolina como inhibidores de PI3K quinasa |
| WO2011058111A1 (en) * | 2009-11-12 | 2011-05-19 | Ucb Pharma S.A. | Aminopurine derivatives as kinase inhibitors |
| WO2011058113A1 (en) * | 2009-11-12 | 2011-05-19 | Ucb Pharma S.A. | Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors |
| CA2784566A1 (en) * | 2009-12-18 | 2011-06-23 | Amgen Inc. | Heterocyclic compounds and their uses |
-
2011
- 2011-06-30 WO PCT/US2011/042519 patent/WO2012003271A1/en not_active Ceased
- 2011-06-30 US US13/703,790 patent/US20130096134A1/en not_active Abandoned
- 2011-06-30 CA CA2803624A patent/CA2803624A1/en not_active Abandoned
- 2011-06-30 AU AU2011272850A patent/AU2011272850A1/en not_active Abandoned
- 2011-06-30 JP JP2013518689A patent/JP2013533884A/ja not_active Withdrawn
- 2011-06-30 EP EP11730846.0A patent/EP2588469A1/en not_active Withdrawn
- 2011-06-30 MX MX2012015134A patent/MX2012015134A/es not_active Application Discontinuation
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