JP2013542941A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013542941A5 JP2013542941A5 JP2013534002A JP2013534002A JP2013542941A5 JP 2013542941 A5 JP2013542941 A5 JP 2013542941A5 JP 2013534002 A JP2013534002 A JP 2013534002A JP 2013534002 A JP2013534002 A JP 2013534002A JP 2013542941 A5 JP2013542941 A5 JP 2013542941A5
- Authority
- JP
- Japan
- Prior art keywords
- membered
- nitrogen
- sulfur
- oxygen
- optionally 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.)
- Pending
Links
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 563
- 229910052757 nitrogen Inorganic materials 0.000 claims description 408
- 229910052760 oxygen Inorganic materials 0.000 claims description 388
- 229910052717 sulfur Inorganic materials 0.000 claims description 383
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 369
- 239000001301 oxygen Substances 0.000 claims description 369
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 363
- 239000011593 sulfur Substances 0.000 claims description 362
- 125000005842 heteroatom Chemical group 0.000 claims description 360
- 229910052739 hydrogen Inorganic materials 0.000 claims description 223
- 125000001931 aliphatic group Chemical group 0.000 claims description 217
- 239000001257 hydrogen Substances 0.000 claims description 213
- 125000000623 heterocyclic group Chemical group 0.000 claims description 205
- 125000002723 alicyclic group Chemical group 0.000 claims description 200
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 163
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 156
- 150000001875 compounds Chemical class 0.000 claims description 145
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 122
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 112
- 150000002431 hydrogen Chemical class 0.000 claims description 78
- 125000002947 alkylene group Chemical group 0.000 claims description 54
- 125000003118 aryl group Chemical group 0.000 claims description 54
- 125000000217 alkyl group Chemical group 0.000 claims description 50
- 229910052736 halogen Inorganic materials 0.000 claims description 44
- 150000002367 halogens Chemical class 0.000 claims description 44
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 125000004429 atom Chemical group 0.000 claims description 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 19
- 125000005843 halogen group Chemical group 0.000 claims description 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 16
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 13
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 11
- 229910052731 fluorine Inorganic materials 0.000 claims description 11
- 239000011737 fluorine Substances 0.000 claims description 11
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 10
- 125000001188 haloalkyl group Chemical group 0.000 claims description 10
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 7
- 101100347605 Arabidopsis thaliana VIII-A gene Proteins 0.000 claims description 5
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims description 3
- 108091007960 PI3Ks Proteins 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- -1 substituted Chemical class 0.000 claims description 3
- 101100347612 Arabidopsis thaliana VIII-B gene Proteins 0.000 claims description 2
- BUDQDWGNQVEFAC-UHFFFAOYSA-N Dihydropyran Chemical compound C1COC=CC1 BUDQDWGNQVEFAC-UHFFFAOYSA-N 0.000 claims description 2
- 101150097381 Mtor gene Proteins 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 13
- 125000004354 sulfur functional group Chemical group 0.000 claims 6
- 238000006467 substitution reaction Methods 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 description 3
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 208000003174 Brain Neoplasms Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 description 1
- 208000006029 Cardiomegaly Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 206010014733 Endometrial cancer Diseases 0.000 description 1
- 206010014759 Endometrial neoplasm Diseases 0.000 description 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 1
- 208000032612 Glial tumor Diseases 0.000 description 1
- 206010018338 Glioma Diseases 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 208000008839 Kidney Neoplasms Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 206010038389 Renal cancer Diseases 0.000 description 1
- 208000005718 Stomach Neoplasms Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 208000024770 Thyroid neoplasm Diseases 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 150000001345 alkine derivatives Chemical class 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- LCIYFINKFGDAHD-UHFFFAOYSA-N azepane;3-nitrobenzoic acid Chemical group C1CCCNCC1.OC(=O)C1=CC=CC([N+]([O-])=O)=C1 LCIYFINKFGDAHD-UHFFFAOYSA-N 0.000 description 1
- 201000010881 cervical cancer Diseases 0.000 description 1
- 208000037976 chronic inflammation Diseases 0.000 description 1
- 230000006020 chronic inflammation Effects 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 201000004101 esophageal cancer Diseases 0.000 description 1
- 206010017758 gastric cancer Diseases 0.000 description 1
- 208000005017 glioblastoma Diseases 0.000 description 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 201000010982 kidney cancer Diseases 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39251510P | 2010-10-13 | 2010-10-13 | |
| US61/392,515 | 2010-10-13 | ||
| PCT/US2011/056135 WO2012051410A2 (en) | 2010-10-13 | 2011-10-13 | Heteroaryls and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013542941A JP2013542941A (ja) | 2013-11-28 |
| JP2013542941A5 true JP2013542941A5 (enExample) | 2014-12-04 |
Family
ID=45938970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013534002A Pending JP2013542941A (ja) | 2010-10-13 | 2011-10-13 | ヘテロアリールおよびその使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US8765746B2 (enExample) |
| EP (1) | EP2627181A4 (enExample) |
| JP (1) | JP2013542941A (enExample) |
| KR (1) | KR20140091462A (enExample) |
| CN (1) | CN103237450A (enExample) |
| AR (1) | AR083450A1 (enExample) |
| AU (1) | AU2011316016A1 (enExample) |
| BR (1) | BR112013009166A2 (enExample) |
| CA (1) | CA2814688A1 (enExample) |
| CL (1) | CL2013001009A1 (enExample) |
| CO (1) | CO6801713A2 (enExample) |
| CR (1) | CR20130204A (enExample) |
| DO (1) | DOP2013000082A (enExample) |
| EA (1) | EA201390539A1 (enExample) |
| EC (1) | ECSP13012621A (enExample) |
| IL (1) | IL225607A0 (enExample) |
| MA (1) | MA34652B1 (enExample) |
| MX (1) | MX2013004003A (enExample) |
| PE (1) | PE20141044A1 (enExample) |
| PH (1) | PH12013500723A1 (enExample) |
| SG (1) | SG189396A1 (enExample) |
| TW (1) | TW201307309A (enExample) |
| UY (1) | UY33671A (enExample) |
| WO (1) | WO2012051410A2 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| US9139589B2 (en) | 2009-01-30 | 2015-09-22 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| MA34797B1 (fr) | 2010-08-11 | 2014-01-02 | Millennium Pharm Inc | Hétéroaryles et leurs utilisations |
| JP2013533318A (ja) | 2010-08-11 | 2013-08-22 | ミレニアム ファーマシューティカルズ， インコーポレイテッド | ヘテロアリールおよびその使用 |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| CN103467481B (zh) * | 2012-06-07 | 2016-08-31 | 上海汇伦生命科技有限公司 | 二氢吡啶类化合物、其组合物、制备方法和用途 |
| WO2016130501A1 (en) | 2015-02-09 | 2016-08-18 | Incyte Corporation | Aza-heteroaryl compounds as pi3k-gamma inhibitors |
| AR106595A1 (es) | 2015-11-06 | 2018-01-31 | Incyte Corp | COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g |
| EP3400221B1 (en) | 2016-01-05 | 2020-08-26 | Incyte Corporation | Pyrazol / imidazol substituted pyridines as pi3k-gamma inhibitors |
| TW201803871A (zh) | 2016-06-24 | 2018-02-01 | 英塞特公司 | 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物 |
| SG11202000864QA (en) | 2017-07-31 | 2020-02-27 | Agency Science Tech & Res | Method of preparing stapled peptides |
| BR112020007593A2 (pt) | 2017-10-18 | 2020-09-24 | Incyte Corporation | derivados de imidazol condensados substituídos por grupos hidróxi terciários como inibidores de pi3k-gama |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| CN110041349B (zh) * | 2019-05-15 | 2021-06-01 | 湖南科技大学 | 一种含螺二氢嘧啶衍生物及其制备方法和应用 |
| CN113966336B (zh) | 2019-06-06 | 2023-11-07 | 和记黄埔医药（上海）有限公司 | 三环类化合物及其用途 |
Family Cites Families (93)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL126440C (enExample) | 1958-08-20 | |||
| US3852293A (en) | 1972-06-21 | 1974-12-03 | Uniroyal Inc | 4-phenyl-2-(3-pyridyl)-thiazole carboxamides |
| US3821384A (en) | 1972-10-06 | 1974-06-28 | Uniroyal Inc | Pharmaceutical compositions containing a4-aryl-2-(3-pyridyl)thiazole and methods of using same |
| DE3021590A1 (de) | 1980-06-09 | 1981-12-17 | Hoechst Ag, 6000 Frankfurt | 4-halogen-5-(halogenmethyl-phenyl)-oxazol-derivate, ein verfahren zu ihrer herstellung und sie enthaltenden strahlungsempfindliche massen |
| DD275870A1 (de) | 1988-09-27 | 1990-02-07 | Univ Leipzig | Verfahren zur herstellung von in 5-position verschiedenartig substituierten 3-aminothiophen-4-carbonitrilen |
| PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| WO1997012613A1 (en) | 1995-10-05 | 1997-04-10 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| WO1998008845A1 (en) | 1996-08-27 | 1998-03-05 | Novartis Ag | Herbicidal s-substituted 1,2,4,6-thiatriazines |
| JPH1087490A (ja) | 1996-09-10 | 1998-04-07 | Sagami Chem Res Center | インターロイキン６生産抑制剤、骨吸収抑制剤、抗骨粗鬆症剤、及びチアゾール化合物 |
| PT853083E (pt) | 1997-01-06 | 2001-12-28 | Pfizer | Composto de piridilfurano e piridiltiofeno e sua utilizacao farmaceutica |
| TR199802691T1 (xx) | 1997-04-24 | 1999-07-21 | Dow Agrosciences Llc | Pestisid etkili 3-(ikameli fenil)-5-(tienil ya da furil)-1,2,4-triazoller |
| JP2002520324A (ja) | 1998-07-10 | 2002-07-09 | メルク エンド カムパニー インコーポレーテッド | 新規な血管形成インヒビター |
| DE19858192A1 (de) | 1998-12-17 | 2000-06-21 | Aventis Cropscience Gmbh | 4-Trifluormethyl-3-oxazolylpyridine, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und ihre Verwendung als Schädlingsbekämpfungsmittel |
| CO5170501A1 (es) | 1999-04-14 | 2002-06-27 | Novartis Ag | AZOLES SUSTITUIDOS UTILES PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR TNFa eIL-1 Y ENFERMEDADES DEL METABOLISMO OSEO |
| NZ520628A (en) | 2000-01-18 | 2004-05-28 | Vertex Pharma | thiazole, oxazole, imdazole or pyrazole substituted pyrazole derivatives useful as treating bacterial infections |
| JP2004535381A (ja) | 2001-04-13 | 2004-11-25 | バーテックス ファーマシューティカルズ インコーポレイテッド | ｃ−ＪｕｎＮ末端キナーゼ（ＪＮＫ）および他のプロテインキナーゼのインヒビター |
| EP1382603B1 (en) | 2001-04-26 | 2008-07-23 | Eisai R&D Management Co., Ltd. | Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof |
| US7405235B2 (en) | 2001-05-04 | 2008-07-29 | Paratek Pharmaceuticals, Inc. | Transcription factor modulating compounds and methods of use thereof |
| US7138403B2 (en) | 2001-08-13 | 2006-11-21 | Janssen Pharmaceutica N.V. | 2,4,5-trisubstituted thiazolyl derivatives and their antiinflammatory activity |
| US7375105B2 (en) | 2001-09-05 | 2008-05-20 | Smithkline Beecham P.L.C. | Pyridine substituted furan derivatives as Raf kinase inhibitors |
| US20040198773A1 (en) | 2001-09-26 | 2004-10-07 | Barry Hart | Substituted 3-pyridyl oxazoles as c17,20 lyase inhibitors |
| WO2003027095A1 (en) | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Substituted 3-pyridyl tetrazoles as steroid c17,20 lyase inhibitors |
| EA200400648A1 (ru) | 2001-11-08 | 2005-04-28 | Элан Фармасьютикалз, Инк. | N, n'-замещенные производные 1,3-диамино-2-гидроксипропана |
| EP1546137A1 (en) | 2002-08-08 | 2005-06-29 | SmithKline Beecham Corporation | Benzimidazol-1-yl-thiophene compounds for the treatment of cancer |
| WO2004016592A1 (en) | 2002-08-14 | 2004-02-26 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| WO2004016741A2 (en) | 2002-08-14 | 2004-02-26 | Ppd Discovery, Inc. | Prenylation inhibitors containing dimethyl-cyclobutane and methods of their synthesis and use |
| TW200519106A (en) | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
| US6984652B2 (en) | 2003-09-05 | 2006-01-10 | Warner-Lambert Company Llc | Gyrase inhibitors |
| US20080293716A1 (en) | 2004-01-30 | 2008-11-27 | Smithkline Beecham Corporation | Chemical Compounds |
| JP2007531757A (ja) | 2004-03-30 | 2007-11-08 | カイロン コーポレイション | 抗癌剤としての置換チオフェン誘導体 |
| EP1742627A4 (en) | 2004-05-06 | 2009-08-26 | Plexxikon Inc | PDE4B HEMMER AND ITS USE |
| GB0423653D0 (en) * | 2004-10-25 | 2004-11-24 | Piramed Ltd | Pharmaceutical compounds |
| EP1831176A2 (en) | 2004-12-21 | 2007-09-12 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| KR101346886B1 (ko) | 2005-01-21 | 2014-01-02 | 아스텍스 테라퓨틱스 리미티드 | 제약 화합물 |
| GB0503962D0 (en) | 2005-02-25 | 2005-04-06 | Kudos Pharm Ltd | Compounds |
| CN1834095B (zh) | 2005-03-18 | 2011-04-20 | 中国科学院上海药物研究所 | 一类非核苷类抗病毒抑制剂及其制备方法和用途 |
| EP1869049B1 (en) | 2005-03-21 | 2009-03-04 | Eli Lilly And Company | Imidazopyridazine compounds |
| GB0508472D0 (en) | 2005-04-26 | 2005-06-01 | Glaxo Group Ltd | Compounds |
| GB0508471D0 (en) * | 2005-04-26 | 2005-06-01 | Celltech R&D Ltd | Therapeutic agents |
| DE102005000046A1 (de) | 2005-04-28 | 2006-11-02 | Voith Patent Gmbh | Maschine zur Herstellung einer Faserstoffbahn |
| MX2008000141A (es) | 2005-06-27 | 2008-04-07 | Exelixis Inc | Moduladores de lxr basados en imidazol. |
| EP1932833B1 (en) | 2005-10-07 | 2012-08-01 | Kissei Pharmaceutical Co., Ltd. | Nitrogenated heterocyclic compound and pharmaceutical composition comprising the same |
| JP2007197324A (ja) | 2006-01-23 | 2007-08-09 | Toray Ind Inc | ２，４，５−置換−１，３−アゾール誘導体 |
| EP1979314B1 (en) | 2006-01-24 | 2013-01-09 | Eli Lilly & Company | Indole sulfonamide modulators of progesterone receptors |
| US7504513B2 (en) | 2006-02-27 | 2009-03-17 | Hoffman-La Roche Inc. | Thiazolyl-benzimidazoles |
| CN101410387B (zh) | 2006-03-27 | 2013-12-18 | 内尔维阿诺医学科学有限公司 | 作为激酶抑制剂的吡啶基-和嘧啶基-取代的吡咯-、噻吩-和呋喃-衍生物 |
| UA95799C2 (en) | 2006-04-26 | 2011-09-12 | Ф. Хоффманн-Ля Рош Аг | Pharmaceutical compounds |
| EP2016075A1 (en) | 2006-05-03 | 2009-01-21 | AstraZeneca AB | Thiazole derivatives and their use as anti-tumour agents |
| EP2027116A2 (en) | 2006-05-23 | 2009-02-25 | Vertex Pharmaceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| WO2007138110A2 (en) | 2006-06-01 | 2007-12-06 | Devgen N.V. | Compounds that interact with ion channels, in particular with ion channels from the kv family |
| EP2035436B1 (en) * | 2006-06-26 | 2011-05-25 | UCB Pharma S.A. | Fused thiazole derivatives as kinase inhibitors |
| CA2658764A1 (en) | 2006-07-20 | 2008-01-24 | Mehmet Kahraman | Benzothiophene inhibitors of rho kinase |
| WO2008014238A2 (en) | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| AU2007284688A1 (en) | 2006-08-14 | 2008-02-21 | Schering Corporation | Process and intermediates for the synthesis of 2-(Quinolin-5-yl)-4,5 Disubstituted-Azole derivatives |
| CA2660758A1 (en) | 2006-08-24 | 2008-02-27 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| WO2008024980A2 (en) | 2006-08-24 | 2008-02-28 | Serenex, Inc. | Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives |
| CN101516886B (zh) | 2006-09-20 | 2012-02-29 | 伊莱利利公司 | 噻吩吡唑并嘧啶化合物 |
| DE602007014256D1 (de) | 2006-12-04 | 2011-06-09 | Astrazeneca Ab | Antibakterielle polycyclische harnstoffverbindungen |
| WO2008083070A1 (en) | 2006-12-29 | 2008-07-10 | Neurogen Corporation | Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties |
| GB0701426D0 (en) | 2007-01-25 | 2007-03-07 | Univ Sheffield | Compounds and their use |
| CA2677264C (en) | 2007-02-02 | 2021-11-30 | Baylor College Of Medicine | Compositions and methods for the treatment of metabolic disorders |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| EP2114388B1 (en) | 2007-02-07 | 2015-05-20 | GlaxoSmithKline LLC | Inhibitors of akt activity |
| AR066348A1 (es) | 2007-04-30 | 2009-08-12 | Genentech Inc | Inhibidores de las iap |
| GB0709031D0 (en) | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
| WO2008157273A1 (en) | 2007-06-14 | 2008-12-24 | Smithkline Beecham Corporation | Chemical compounds |
| WO2009006577A2 (en) | 2007-07-03 | 2009-01-08 | The Regents Of The University Of Michigan | Compositions and methods for inhibiting ezh2 |
| US8067613B2 (en) | 2007-07-16 | 2011-11-29 | Abbott Laboratories | Benzimidazole poly(ADP ribose)polymerase inhibitors |
| WO2009040730A2 (en) | 2007-09-24 | 2009-04-02 | Actelion Pharmaceuticals Ltd | Pyrrolidines and piperidines as orexin receptor antagonists |
| ES2399774T3 (es) | 2007-09-24 | 2013-04-03 | Genentech, Inc. | Compuestos de tiazolopirimidina inhibidores de PI3K y métodos de uso |
| WO2009049028A1 (en) | 2007-10-09 | 2009-04-16 | Targegen Inc. | Pyrrolopyrimidine compounds and their use as janus kinase modulators |
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| TW200940537A (en) | 2008-02-26 | 2009-10-01 | Astrazeneca Ab | Heterocyclic urea derivatives and methods of use thereof |
| GB0805818D0 (en) * | 2008-03-31 | 2008-04-30 | Ucb Pharma Sa | Therapeutic agents |
| RU2506267C2 (ru) * | 2008-03-31 | 2014-02-10 | Дженентек, Инк. | Бензопирановые и бензоксепиновые ингибиторы рi3k и их применение |
| CN102066365A (zh) | 2008-06-19 | 2011-05-18 | 米伦纽姆医药公司 | 噻吩或噻唑衍生物和其作为pi3k抑制剂的用途 |
| WO2009158374A2 (en) | 2008-06-26 | 2009-12-30 | Smithkline Beecham Corporation | Inhibitors of akt activity |
| GB0812309D0 (en) | 2008-07-03 | 2008-08-13 | Ucb Pharma Sa | Therapeutic agents |
| WO2010005841A1 (en) | 2008-07-09 | 2010-01-14 | Merck & Co., Inc. | Inhibitors of janus kinases |
| WO2010017079A1 (en) | 2008-08-04 | 2010-02-11 | Merck & Co., Inc. | Oxazole derivatives useful as inhibitors of faah |
| JP5877064B2 (ja) | 2008-11-11 | 2016-03-02 | エックスカバリー ホールディング カンパニー エルエルシー | ＰＩ３Ｋ／ｍＴＯＲキナーゼ阻害剤 |
| GB0820819D0 (en) | 2008-11-13 | 2008-12-24 | Sareum Ltd | Pharmaceutical compounds |
| WO2010080873A1 (en) | 2009-01-08 | 2010-07-15 | Glaxo Group Limited | Oxazoles as modulators of chemokine receptors |
| US9139589B2 (en) | 2009-01-30 | 2015-09-22 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| EP2430013B1 (en) | 2009-05-13 | 2014-10-15 | Amgen Inc. | Heteroaryl compounds as pikk inhibitors |
| US20110021531A1 (en) | 2009-07-27 | 2011-01-27 | Chobanian Harry | Oxazole derivatives useful as inhibitors of faah |
| JP2012254939A (ja) | 2009-10-07 | 2012-12-27 | Astellas Pharma Inc | オキサゾール化合物 |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| JP2013533318A (ja) | 2010-08-11 | 2013-08-22 | ミレニアム ファーマシューティカルズ， インコーポレイテッド | ヘテロアリールおよびその使用 |
| MA34797B1 (fr) | 2010-08-11 | 2014-01-02 | Millennium Pharm Inc | Hétéroaryles et leurs utilisations |
| US20130165472A1 (en) | 2011-12-23 | 2013-06-27 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
-
2011
- 2011-10-13 PH PH1/2013/500723A patent/PH12013500723A1/en unknown
- 2011-10-13 SG SG2013027958A patent/SG189396A1/en unknown
- 2011-10-13 KR KR1020137012227A patent/KR20140091462A/ko not_active Withdrawn
- 2011-10-13 JP JP2013534002A patent/JP2013542941A/ja active Pending
- 2011-10-13 WO PCT/US2011/056135 patent/WO2012051410A2/en not_active Ceased
- 2011-10-13 CN CN2011800586347A patent/CN103237450A/zh active Pending
- 2011-10-13 MX MX2013004003A patent/MX2013004003A/es not_active Application Discontinuation
- 2011-10-13 BR BR112013009166A patent/BR112013009166A2/pt not_active IP Right Cessation
- 2011-10-13 AR ARP110103813A patent/AR083450A1/es unknown
- 2011-10-13 CA CA2814688A patent/CA2814688A1/en not_active Abandoned
- 2011-10-13 US US13/272,413 patent/US8765746B2/en active Active
- 2011-10-13 EA EA201390539A patent/EA201390539A1/ru unknown
- 2011-10-13 TW TW100137181A patent/TW201307309A/zh unknown
- 2011-10-13 PE PE2013000845A patent/PE20141044A1/es not_active Application Discontinuation
- 2011-10-13 EP EP11833402.8A patent/EP2627181A4/en not_active Withdrawn
- 2011-10-13 AU AU2011316016A patent/AU2011316016A1/en not_active Abandoned
- 2011-10-13 UY UY0001033671A patent/UY33671A/es not_active Application Discontinuation
-
2013
- 2013-04-07 IL IL225607A patent/IL225607A0/en unknown
- 2013-04-12 CL CL2013001009A patent/CL2013001009A1/es unknown
- 2013-04-16 DO DO2013000082A patent/DOP2013000082A/es unknown
- 2013-05-06 MA MA35882A patent/MA34652B1/fr unknown
- 2013-05-08 CR CR20130204A patent/CR20130204A/es unknown
- 2013-05-10 CO CO13117641A patent/CO6801713A2/es not_active Application Discontinuation
- 2013-05-13 EC ECSP13012621 patent/ECSP13012621A/es unknown
-
2014
- 2014-06-27 US US14/318,223 patent/US20150148334A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013542941A5 (enExample) | ||
| ME02630B (me) | Makrociklički derivati, namijenjeni liječenju proliferativnih bolesti | |
| RU2013139353A (ru) | Трициклические пирролопроизводные, способ их получения и их применение в качестве ингибиторов киназы | |
| JP2012520861A5 (enExample) | ||
| JP2011500623A5 (enExample) | ||
| JP2019517487A5 (enExample) | ||
| JP2015503504A5 (enExample) | ||
| AU2015306662A1 (en) | Compounds and methods for inhibiting histone demethylases | |
| JP2018520195A5 (enExample) | ||
| JP2004509114A5 (enExample) | ||
| JP2015503505A5 (enExample) | ||
| JP2014503567A5 (enExample) | ||
| RU2014141579A (ru) | Гетероциклические соединения в качестве ингибиторов бета-лактамаз | |
| JP2013544261A5 (enExample) | ||
| CA2422299A1 (en) | Triazole compounds useful as protein kinase inhibitors | |
| ME02561B (me) | Supstituisani 4-fenil-piridini za terapiju bolesti povezanih sa nk- 1 receptorom | |
| NO20082101L (no) | Pyrido-, pyrazo- og pyrimido-pyrimidinderivater som mTor inhibitorer | |
| BRPI0519794A2 (pt) | derivados de [4-(heteroaril)piperazin-1-il]-(fenil 2,5-substituìdo)metanona como inibidores de transportador de glicina 1 (glyt-1) para o tratamento de distúrbios neurológicos e neuropsiquiátricos | |
| JP2020515583A5 (enExample) | ||
| RU2015124002A (ru) | Соединения, применяемые в качестве ингибиторов индоламин-2,3-диоксигеназы | |
| CA2954999C (en) | Fused quinoline compounds as pi3k, mtor inhibitors | |
| RU2013148405A (ru) | Ингибиторы киназ | |
| JP2019500315A5 (enExample) | ||
| RU2015116749A (ru) | Антагонисты mglu2/3 для лечения аутических расстройств | |
| RU98115533A (ru) | Новые производные бензоилгуанидина, способ их получения и их применение при получении лекарственных средств |