JP2013530238A5 - - Google Patents
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- Publication number
- JP2013530238A5 JP2013530238A5 JP2013518692A JP2013518692A JP2013530238A5 JP 2013530238 A5 JP2013530238 A5 JP 2013530238A5 JP 2013518692 A JP2013518692 A JP 2013518692A JP 2013518692 A JP2013518692 A JP 2013518692A JP 2013530238 A5 JP2013530238 A5 JP 2013530238A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- haloalkyl
- halo
- substituted
- cyano
- 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- Withdrawn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 115
- 125000005843 halogen group Chemical group 0.000 claims 23
- 125000004093 cyano group Chemical group *C#N 0.000 claims 17
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 229920006395 saturated elastomer Polymers 0.000 claims 9
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 230000002757 inflammatory effect Effects 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000000464 thioxo group Chemical group S=* 0.000 claims 4
- 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
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000002950 monocyclic group Chemical group 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
- 206010027654 Allergic conditions Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 206010048768 Dermatosis 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
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000004681 Psoriasis 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
- 201000010099 disease Diseases 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
- 230000001404 mediated effect Effects 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
- 238000006467 substitution reaction Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36073110P | 2010-07-01 | 2010-07-01 | |
| US61/360,731 | 2010-07-01 | ||
| PCT/US2011/042525 WO2012003274A1 (en) | 2010-07-01 | 2011-06-30 | Heterocyclic compounds and their use as inhibitors of pi3k activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013530238A JP2013530238A (ja) | 2013-07-25 |
| JP2013530238A5 true JP2013530238A5 (https=) | 2014-08-14 |
Family
ID=44280219
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013518692A Withdrawn JP2013530238A (ja) | 2010-07-01 | 2011-06-30 | Ｐｉ３ｋ活性の阻害剤としての複素環化合物及びその使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20130085131A1 (https=) |
| EP (1) | EP2588467A1 (https=) |
| JP (1) | JP2013530238A (https=) |
| AU (1) | AU2011272853A1 (https=) |
| CA (1) | CA2803009A1 (https=) |
| MX (1) | MX2012015135A (https=) |
| WO (1) | WO2012003274A1 (https=) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG176986A1 (en) * | 2009-06-25 | 2012-02-28 | Amgen Inc | Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases |
| KR101763656B1 (ko) | 2009-06-29 | 2017-08-01 | 인사이트 홀딩스 코포레이션 | Ｐｉ3ｋ 저해물질로서의 피리미디논 |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| 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 |
| CA2799579A1 (en) | 2010-05-21 | 2011-11-24 | Intellikine, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| EP3660016A1 (en) | 2010-12-20 | 2020-06-03 | Incyte Holdings Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | 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 |
| MX2014002542A (es) | 2011-08-29 | 2014-07-09 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos y usos de los mismos. |
| PT3513793T (pt) | 2011-09-02 | 2021-05-10 | Incyte Holdings Corp | Heterociclilaminas como inibidores de pi3k |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| AU2013343105B2 (en) | 2012-11-08 | 2016-04-14 | Pfizer Inc. | Heteroaromatic compounds as dopamine D1 ligands |
| 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 |
| AU2013364068B2 (en) | 2012-12-21 | 2016-10-20 | Gilead Calistoga Llc | Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors |
| JP6207100B2 (ja) | 2012-12-21 | 2017-10-04 | ギリアード カリストガ エルエルシー | イソキノリノンまたはキナゾリノンホスファチジルイノシトール３−キナーゼ阻害剤 |
| 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 |
| PL3008053T3 (pl) | 2013-06-14 | 2018-08-31 | Gilead Calistoga Llc | Inhibitory 3-kinazy fosfatydyloinozytolu |
| SG11201608943VA (en) * | 2014-04-30 | 2016-11-29 | Univ Columbia | Substituted 4-phenylpiperidines, their preparaiton and use |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| HK1232227A1 (zh) | 2014-07-04 | 2018-01-05 | Lupin Limited | 作为pi3k抑制剂的喹嗪酮衍生物 |
| KR102431436B1 (ko) | 2014-08-29 | 2022-08-10 | 테스 파마 에스.알.엘. | α-아미노-β-카복시뮤콘산 세미알데히드 데카복실라제의 억제제 |
| JP6399518B2 (ja) * | 2014-12-18 | 2018-10-03 | インターナショナル・ビジネス・マシーンズ・コーポレーションＩｎｔｅｒｎａｔｉｏｎａｌ Ｂｕｓｉｎｅｓｓ Ｍａｃｈｉｎｅｓ Ｃｏｒｐｏｒａｔｉｏｎ | 処理装置、処理方法、およびプログラム |
| SG10201907576SA (en) | 2015-02-27 | 2019-09-27 | Incyte Corp | Salts of pi3k 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 |
| 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 |
| 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 |
| 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 |
| SG11202011680YA (en) | 2018-06-01 | 2020-12-30 | Incyte Corp | Dosing regimen for the treatment of pi3k related disorders |
| PT4426434T (pt) | 2021-11-02 | 2025-11-24 | Flare Therapeutics Inc | Agonistas inversos de pparg e suas utilizações |
Family Cites Families (14)
| 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 |
| US20070015782A1 (en) | 2005-04-15 | 2007-01-18 | Eisai Co., Ltd. | Benzimidazole compound |
| TWI510598B (zh) | 2007-03-08 | 2015-12-01 | Universal Display Corp | 磷光材料 |
| DK2137186T3 (en) * | 2007-03-23 | 2016-04-18 | Amgen Inc | Heterocyclic compounds and their uses |
| EP2139882B1 (en) * | 2007-03-23 | 2013-12-25 | Amgen Inc. | 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| EP2155194B1 (en) | 2007-04-06 | 2015-01-21 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| US8367702B2 (en) * | 2007-09-26 | 2013-02-05 | Astellas Pharma Inc. | Quinolone derivative |
| SG176986A1 (en) * | 2009-06-25 | 2012-02-28 | Amgen Inc | Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases |
| EP2499126B1 (en) * | 2009-11-12 | 2015-01-07 | UCB Pharma, S.A. | Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors |
| MX2012006953A (es) * | 2009-12-18 | 2012-10-09 | Amgen Inc | Compuestos heterociclicos y sus usos. |
-
2011
- 2011-06-30 US US13/702,368 patent/US20130085131A1/en not_active Abandoned
- 2011-06-30 AU AU2011272853A patent/AU2011272853A1/en not_active Abandoned
- 2011-06-30 MX MX2012015135A patent/MX2012015135A/es not_active Application Discontinuation
- 2011-06-30 EP EP11730534.2A patent/EP2588467A1/en not_active Withdrawn
- 2011-06-30 WO PCT/US2011/042525 patent/WO2012003274A1/en not_active Ceased
- 2011-06-30 CA CA2803009A patent/CA2803009A1/en not_active Abandoned
- 2011-06-30 JP JP2013518692A patent/JP2013530238A/ja not_active Withdrawn
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