JP2013530238A - Pi3k活性の阻害剤としての複素環化合物及びその使用 - Google Patents
Pi3k活性の阻害剤としての複素環化合物及びその使用 Download PDFInfo
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- JP2013530238A JP2013530238A JP2013518692A JP2013518692A JP2013530238A JP 2013530238 A JP2013530238 A JP 2013530238A JP 2013518692 A JP2013518692 A JP 2013518692A JP 2013518692 A JP2013518692 A JP 2013518692A JP 2013530238 A JP2013530238 A JP 2013530238A
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- Prior art keywords
- alkyl
- amino
- haloalkyl
- ethyl
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- 0 *C(*)(*C(I)=**=*C(*)=*)c1nc(****2)c2c(*)c1I Chemical compound *C(*)(*C(I)=**=*C(*)=*)c1nc(****2)c2c(*)c1I 0.000 description 8
- IGFWVSIGFQOPTE-UHFFFAOYSA-N CC(c1c(C2CC2)c(OC)c(cc(cc2)F)c2n1)N(C(c1ccccc11)=O)C1=O Chemical compound CC(c1c(C2CC2)c(OC)c(cc(cc2)F)c2n1)N(C(c1ccccc11)=O)C1=O IGFWVSIGFQOPTE-UHFFFAOYSA-N 0.000 description 2
- ASTDKNJEDKQYQQ-UHFFFAOYSA-N CC(c1c(C2CC2)c(OC)c(cc(cc2)F)c2n1)Nc1ncnc(N)c1C#N Chemical compound CC(c1c(C2CC2)c(OC)c(cc(cc2)F)c2n1)Nc1ncnc(N)c1C#N ASTDKNJEDKQYQQ-UHFFFAOYSA-N 0.000 description 2
- OQNQSYVHGUXDNM-UHFFFAOYSA-N CC(C)Oc1c(C(N(C)C)=O)c(cc(cc2)F)c2nc1C(C)Nc1ncnc(N)c1C#N Chemical compound CC(C)Oc1c(C(N(C)C)=O)c(cc(cc2)F)c2nc1C(C)Nc1ncnc(N)c1C#N OQNQSYVHGUXDNM-UHFFFAOYSA-N 0.000 description 1
- KIFSSYJLDUQHDI-UHFFFAOYSA-N CC(c(nc(ccc(F)c1)c1c1OC)c1Br)N(C(c1c2cccc1)=O)C2=O Chemical compound CC(c(nc(ccc(F)c1)c1c1OC)c1Br)N(C(c1c2cccc1)=O)C2=O KIFSSYJLDUQHDI-UHFFFAOYSA-N 0.000 description 1
- IWMWYLJBOSCYFK-UHFFFAOYSA-N CC(c1nc(ccc(F)c2)c2c(C(N(C2)CC2N)=O)c1OC)Nc1ncnc(N)c1C#N Chemical compound CC(c1nc(ccc(F)c2)c2c(C(N(C2)CC2N)=O)c1OC)Nc1ncnc(N)c1C#N IWMWYLJBOSCYFK-UHFFFAOYSA-N 0.000 description 1
- IDHRGNLSOGKOHF-UHFFFAOYSA-N CC(c1nc(ccc(F)c2)c2c(OC)c1Br)Br Chemical compound CC(c1nc(ccc(F)c2)c2c(OC)c1Br)Br IDHRGNLSOGKOHF-UHFFFAOYSA-N 0.000 description 1
- NIEOPVRHOFRLQI-UHFFFAOYSA-N CCN(CC)Cc1c(CNc2ncnc(N)c2C#N)nc(cccc2F)c2c1 Chemical compound CCN(CC)Cc1c(CNc2ncnc(N)c2C#N)nc(cccc2F)c2c1 NIEOPVRHOFRLQI-UHFFFAOYSA-N 0.000 description 1
- AUCXFLULRQIGPB-JTQLQIEISA-N CCNC(c1c([C@H](C)Nc2ncnc(N)c2C#N)nc(ccc(F)c2)c2c1)=O Chemical compound CCNC(c1c([C@H](C)Nc2ncnc(N)c2C#N)nc(ccc(F)c2)c2c1)=O AUCXFLULRQIGPB-JTQLQIEISA-N 0.000 description 1
- STFDKZZMZZQYGQ-JTQLQIEISA-N CCOc1c(C(NC)=O)c(cc(cc2)F)c2nc1[C@H](C)Nc1ncnc(N)c1C#N Chemical compound CCOc1c(C(NC)=O)c(cc(cc2)F)c2nc1[C@H](C)Nc1ncnc(N)c1C#N STFDKZZMZZQYGQ-JTQLQIEISA-N 0.000 description 1
- LLDWHOHWGSXIEA-UHFFFAOYSA-N CCc(nc(ccc(F)c1)c1c1OC)c1Br Chemical compound CCc(nc(ccc(F)c1)c1c1OC)c1Br LLDWHOHWGSXIEA-UHFFFAOYSA-N 0.000 description 1
- ASTDKNJEDKQYQQ-JTQLQIEISA-N C[C@@H](c(c(C1CC1)c(c1c2)OC)nc1ccc2F)Nc1ncnc(N)c1C#N Chemical compound C[C@@H](c(c(C1CC1)c(c1c2)OC)nc1ccc2F)Nc1ncnc(N)c1C#N ASTDKNJEDKQYQQ-JTQLQIEISA-N 0.000 description 1
- YADWDROEOBMCGD-NSHDSACASA-N C[C@@H](c(nc(cccc1F)c1c1)c1C(NCC1CC1)=O)Nc1ncnc(N)c1C#N Chemical compound C[C@@H](c(nc(cccc1F)c1c1)c1C(NCC1CC1)=O)Nc1ncnc(N)c1C#N YADWDROEOBMCGD-NSHDSACASA-N 0.000 description 1
- GFDWQQXDAKRNJQ-ZDUSSCGKSA-N C[C@@H](c(nc(cccc1F)c1c1)c1C(NCC1CCOCC1)=O)Nc1ncnc(N)c1C#N Chemical compound C[C@@H](c(nc(cccc1F)c1c1)c1C(NCC1CCOCC1)=O)Nc1ncnc(N)c1C#N GFDWQQXDAKRNJQ-ZDUSSCGKSA-N 0.000 description 1
- BUYHUAHJVTZMNA-NSHDSACASA-N C[C@@H](c(nc1c(F)cccc1c1)c1C(NCCS(C)(=O)=O)=O)Nc1ncnc(N)c1C#N Chemical compound C[C@@H](c(nc1c(F)cccc1c1)c1C(NCCS(C)(=O)=O)=O)Nc1ncnc(N)c1C#N BUYHUAHJVTZMNA-NSHDSACASA-N 0.000 description 1
- ASTDKNJEDKQYQQ-SNVBAGLBSA-N C[C@H](c(c(C1CC1)c(c1c2)OC)nc1ccc2F)Nc(ncnc1N)c1C#N Chemical compound C[C@H](c(c(C1CC1)c(c1c2)OC)nc1ccc2F)Nc(ncnc1N)c1C#N ASTDKNJEDKQYQQ-SNVBAGLBSA-N 0.000 description 1
- PHBLZACTWWFAER-UHFFFAOYSA-N Nc1cccc(F)c1CO Chemical compound Nc1cccc(F)c1CO PHBLZACTWWFAER-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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 true JP2013530238A (ja) | 2013-07-25 |
| JP2013530238A5 JP2013530238A5 (enExample) | 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 (enExample) |
| EP (1) | EP2588467A1 (enExample) |
| JP (1) | JP2013530238A (enExample) |
| AU (1) | AU2011272853A1 (enExample) |
| CA (1) | CA2803009A1 (enExample) |
| MX (1) | MX2012015135A (enExample) |
| WO (1) | WO2012003274A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013527123A (ja) * | 2009-06-25 | 2013-06-27 | アムジエン・インコーポレーテツド | ピリジンの多環式誘導体ならびに(とりわけ)リウマチ性関節炎および同様の疾患の治療におけるそれらの使用 |
| JP2018507222A (ja) * | 2015-03-06 | 2018-03-15 | 南京▲聖▼和▲薬業▼股▲ふん▼有限公司Nanjing Sanhome Pharmaceutical Co., Ltd. | ホスファチジルイノシトール3−キナーゼδ阻害剤としての置換ピリミジン化合物及びその使用 |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2011013816A (es) | 2009-06-29 | 2012-04-11 | Incyte Corp | Pirimidinonas como inhibidores de pi3k. |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone 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 |
| AU2011255218B2 (en) | 2010-05-21 | 2015-03-12 | Infinity Pharmaceuticals, 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 |
| ES2764848T3 (es) | 2010-12-20 | 2020-06-04 | Incyte Holdings Corp | N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| 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 |
| SG10201601516QA (en) | 2011-01-21 | 2016-03-30 | Eisai R&D Man Co Ltd | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | 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 |
| HK1199725A1 (en) | 2011-08-29 | 2015-07-17 | 无限药品股份有限公司 | 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 |
| 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 |
| GEP201606598B (en) | 2012-11-08 | 2017-01-10 | Pfizer | Heteroaromatic compounds as dopamine d1 ligands |
| AU2013364068B2 (en) | 2012-12-21 | 2016-10-20 | Gilead Calistoga Llc | Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors |
| US9029384B2 (en) | 2012-12-21 | 2015-05-12 | Gilead Calistoga, LLC. | 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 |
| BR112015031475A2 (pt) | 2013-06-14 | 2017-07-25 | Gilead Sciences Inc | composto, composição farmacêutica, método para tratamento de uma doença ou condição, kit, e, uso de composto. |
| SG11201608943VA (en) * | 2014-04-30 | 2016-11-29 | Univ Columbia | Substituted 4-phenylpiperidines, their preparaiton and use |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| MA40250A (fr) | 2014-07-04 | 2017-05-10 | Lupin Ltd | Dérivés de quinolizinone utilisés comme inhibiteurs de pi3k |
| ES2901114T3 (es) | 2014-08-29 | 2022-03-21 | Tes Pharma S R L | Inhibidores de ácido alfa-amino-beta-carboximucónico semialdehído descarboxilasa |
| 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 |
| AU2016222556B2 (en) | 2015-02-27 | 2020-08-27 | Incyte Holdings Corporation | Salts of Pl3K inhibitor and processes for their preparation |
| 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 |
| 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 |
| MX2020012826A (es) | 2018-06-01 | 2021-03-09 | Incyte Corp | Regimen de dosificacion para el tratamiento de trastornos relacionados con fosfatidilinositol 3-cinasas (pi3k). |
| TW202334089A (zh) | 2021-11-02 | 2023-09-01 | 美商夫雷爾醫療公司 | Pparg反向激動劑及其用途 |
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| 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 |
| TWI573854B (zh) | 2007-03-08 | 2017-03-11 | 環球展覽公司 | 磷光材料 |
| HUE028954T2 (en) * | 2007-03-23 | 2017-01-30 | Amgen Inc | Heterocyclic compounds and their use |
| PT2139882E (pt) * | 2007-03-23 | 2014-01-30 | Amgen Inc | Derivados de quinolina ou quinoxalina 3-substituídos e sua utilização como inibidores de fosfatidilinositol 3-cinase (pi3k) |
| PE20090044A1 (es) | 2007-04-06 | 2009-01-23 | Neurocrine Biosciences Inc | Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos |
| CA2700088A1 (en) * | 2007-09-26 | 2009-04-02 | Astellas Pharma Inc. | Quinolone derivative |
| EP2445900B1 (en) * | 2009-06-25 | 2016-03-02 | Amgen, Inc | Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases |
| WO2011058113A1 (en) * | 2009-11-12 | 2011-05-19 | Ucb Pharma S.A. | Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors |
| WO2011075628A1 (en) * | 2009-12-18 | 2011-06-23 | Amgen Inc. | Heterocyclic compounds and their uses |
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- 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 EP EP11730534.2A patent/EP2588467A1/en not_active Withdrawn
- 2011-06-30 CA CA2803009A patent/CA2803009A1/en not_active Abandoned
- 2011-06-30 WO PCT/US2011/042525 patent/WO2012003274A1/en not_active Ceased
- 2011-06-30 MX MX2012015135A patent/MX2012015135A/es not_active Application Discontinuation
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013527123A (ja) * | 2009-06-25 | 2013-06-27 | アムジエン・インコーポレーテツド | ピリジンの多環式誘導体ならびに(とりわけ)リウマチ性関節炎および同様の疾患の治療におけるそれらの使用 |
| JP2018507222A (ja) * | 2015-03-06 | 2018-03-15 | 南京▲聖▼和▲薬業▼股▲ふん▼有限公司Nanjing Sanhome Pharmaceutical Co., Ltd. | ホスファチジルイノシトール3−キナーゼδ阻害剤としての置換ピリミジン化合物及びその使用 |
| US10077258B2 (en) | 2015-03-06 | 2018-09-18 | Nanjing Sanhome Pharmaceutical Co., Ltd. | Substituted pyrimidine compounds as phosphatidylinositol 3-kinase delta inhibitor and use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2012015135A (es) | 2013-05-06 |
| CA2803009A1 (en) | 2012-01-05 |
| US20130085131A1 (en) | 2013-04-04 |
| EP2588467A1 (en) | 2013-05-08 |
| AU2011272853A1 (en) | 2013-01-10 |
| WO2012003274A1 (en) | 2012-01-05 |
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