JP2013533318A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013533318A5 JP2013533318A5 JP2013524201A JP2013524201A JP2013533318A5 JP 2013533318 A5 JP2013533318 A5 JP 2013533318A5 JP 2013524201 A JP2013524201 A JP 2013524201A JP 2013524201 A JP2013524201 A JP 2013524201A JP 2013533318 A5 JP2013533318 A5 JP 2013533318A5
- Authority
- JP
- Japan
- Prior art keywords
- membered
- optionally substituted
- nitrogen
- oxygen
- sulfur
- 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 146
- 229910052757 nitrogen Inorganic materials 0.000 claims description 100
- 229910052760 oxygen Inorganic materials 0.000 claims description 98
- 229910052717 sulfur Inorganic materials 0.000 claims description 93
- 125000005842 heteroatom Chemical group 0.000 claims description 89
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 88
- 239000001301 oxygen Substances 0.000 claims description 88
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 84
- 239000011593 sulfur Substances 0.000 claims description 83
- 150000001875 compounds Chemical class 0.000 claims description 78
- 125000002723 alicyclic group Chemical group 0.000 claims description 60
- 125000001931 aliphatic group Chemical group 0.000 claims description 60
- 125000000623 heterocyclic group Chemical group 0.000 claims description 55
- 229910052739 hydrogen Inorganic materials 0.000 claims description 50
- 239000001257 hydrogen Substances 0.000 claims description 50
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 35
- 125000003118 aryl group Chemical group 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 32
- 150000002367 halogens Chemical class 0.000 claims description 32
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 22
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 21
- -1 4-pyridinyl Chemical group 0.000 claims description 18
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 16
- 125000002947 alkylene group Chemical group 0.000 claims description 16
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 16
- 125000000217 alkyl group Chemical group 0.000 claims description 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 150000002431 hydrogen Chemical group 0.000 claims description 9
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 8
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 6
- 150000004702 methyl esters Chemical class 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims description 5
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 4
- VAELWSLNTRVXQS-UHFFFAOYSA-N 1,3-oxazole-4-carboxamide Chemical compound NC(=O)C1=COC=N1 VAELWSLNTRVXQS-UHFFFAOYSA-N 0.000 claims description 4
- JBCFJMYPJJWIRG-UHFFFAOYSA-N 1,3-oxazole-4-carboxylic acid Chemical compound OC(=O)C1=COC=N1 JBCFJMYPJJWIRG-UHFFFAOYSA-N 0.000 claims description 4
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 4
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 4
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims description 4
- 239000005711 Benzoic acid Substances 0.000 claims description 4
- SIOXPEMLGUPBBT-UHFFFAOYSA-N Picolinic acid Natural products OC(=O)C1=CC=CC=N1 SIOXPEMLGUPBBT-UHFFFAOYSA-N 0.000 claims description 4
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims description 4
- 235000010233 benzoic acid Nutrition 0.000 claims description 4
- 125000004494 ethyl ester group Chemical group 0.000 claims description 4
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- VXKWYPOMXBVZSJ-UHFFFAOYSA-N tetramethyltin Chemical compound C[Sn](C)(C)C VXKWYPOMXBVZSJ-UHFFFAOYSA-N 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 230000002757 inflammatory effect Effects 0.000 claims description 3
- 230000002062 proliferating effect Effects 0.000 claims description 3
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims description 2
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 2
- VYIBCOSBNVFEIW-UHFFFAOYSA-N 3-phenylpropanamide Chemical compound NC(=O)CCC1=CC=CC=C1 VYIBCOSBNVFEIW-UHFFFAOYSA-N 0.000 claims description 2
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims description 2
- 101000605630 Homo sapiens Phosphatidylinositol 3-kinase catalytic subunit type 3 Proteins 0.000 claims description 2
- 108091007960 PI3Ks Proteins 0.000 claims description 2
- 102100038329 Phosphatidylinositol 3-kinase catalytic subunit type 3 Human genes 0.000 claims description 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 2
- 125000001246 bromo group Chemical group Br* 0.000 claims description 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 2
- VLTRZXGMWDSKGL-UHFFFAOYSA-M perchlorate Inorganic materials [O-]Cl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-M 0.000 claims description 2
- VLTRZXGMWDSKGL-UHFFFAOYSA-N perchloric acid Chemical compound OCl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-N 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- JEXVQSWXXUJEMA-UHFFFAOYSA-N pyrazol-3-one Chemical compound O=C1C=CN=N1 JEXVQSWXXUJEMA-UHFFFAOYSA-N 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-O pyridinium Chemical compound C1=CC=[NH+]C=C1 JUJWROOIHBZHMG-UHFFFAOYSA-O 0.000 claims description 2
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000004354 sulfur functional group Chemical group 0.000 claims 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 208000035475 disorder Diseases 0.000 description 2
- 125000001188 haloalkyl group Chemical group 0.000 description 2
- 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
- 208000038016 acute inflammation Diseases 0.000 description 1
- 230000006022 acute inflammation Effects 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
- 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
- 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
- 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
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 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 (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37262810P | 2010-08-11 | 2010-08-11 | |
| US37255310P | 2010-08-11 | 2010-08-11 | |
| US61/372,628 | 2010-08-11 | ||
| US61/372,553 | 2010-08-11 | ||
| US201161469157P | 2011-03-30 | 2011-03-30 | |
| US61/469,157 | 2011-03-30 | ||
| PCT/US2011/047245 WO2012021615A1 (en) | 2010-08-11 | 2011-08-10 | Heteroaryls and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013533318A JP2013533318A (ja) | 2013-08-22 |
| JP2013533318A5 true JP2013533318A5 (enExample) | 2014-09-25 |
Family
ID=45567934
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013524201A Pending JP2013533318A (ja) | 2010-08-11 | 2011-08-10 | ヘテロアリールおよびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8859768B2 (enExample) |
| EP (1) | EP2603216A4 (enExample) |
| JP (1) | JP2013533318A (enExample) |
| AR (1) | AR082666A1 (enExample) |
| TW (1) | TW201217362A (enExample) |
| WO (1) | WO2012021615A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes 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 |
| US9139589B2 (en) | 2009-01-30 | 2015-09-22 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MA34797B1 (fr) | 2010-08-11 | 2014-01-02 | Millennium Pharm Inc | Hétéroaryles et leurs utilisations |
| WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2012051410A2 (en) | 2010-10-13 | 2012-04-19 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MA37830B1 (fr) | 2012-08-10 | 2018-09-28 | Boehringer Ingelheim Int | Composés hétéroromatiques en tant qu'inhibiteurs de la tyrosine kinase de bruton (btk) |
| WO2015108861A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9828364B2 (en) | 2014-01-29 | 2017-11-28 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as BTK inhibitors |
| EP3156405A1 (en) | 2015-10-13 | 2017-04-19 | Boehringer Ingelheim International GmbH | Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide |
| PE20181074A1 (es) | 2015-12-16 | 2018-07-04 | Boehringer Ingelheim Int | Compuestos heteroaromaticos como inhibidores de btk |
| US10570118B2 (en) | 2016-01-13 | 2020-02-25 | Boehringer Ingelheim International Gmbh | Isoquinolones as BTK inhibitors |
| WO2025054366A1 (en) * | 2023-09-06 | 2025-03-13 | Nico Therapeutics, Inc. | Compounds, compositions, and methods |
Family Cites Families (94)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL242505A (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 |
| US6268308B1 (en) | 1996-08-27 | 2001-07-31 | Syngenta Crop Protection, Inc. | 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 |
| JP4306806B2 (ja) | 1997-04-24 | 2009-08-05 | ダウ・アグロサイエンス・エル・エル・シー | 有害生物防除性 ３―（置換フェニル）―５―（チエニルまたはフリル）―１，２，４―トリアゾール |
| CA2336848A1 (en) * | 1998-07-10 | 2000-01-20 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| 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 |
| AU782883B2 (en) | 2000-01-18 | 2005-09-08 | Vertex Pharmaceuticals Incorpoated | Gyrase inhibitors and uses thereof |
| 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 |
| JP4310109B2 (ja) | 2001-04-26 | 2009-08-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピラゾリル基を置換基として有する含窒素縮合環化合物およびその医薬組成物 |
| US7405235B2 (en) | 2001-05-04 | 2008-07-29 | Paratek Pharmaceuticals, Inc. | Transcription factor modulating compounds and methods of use thereof |
| WO2003015776A1 (en) | 2001-08-13 | 2003-02-27 | Janssen Pharmaceutica N.V. | 2,4,5-trisubstituted thiazolyl derivatives and their antiinflammatory activity |
| DE60228098D1 (de) * | 2001-09-05 | 2008-09-18 | Smithkline Beecham Plc | Pyridin-substituierte furanderivate als raf-kinase inhibitoren |
| US20040198773A1 (en) | 2001-09-26 | 2004-10-07 | Barry Hart | Substituted 3-pyridyl oxazoles as c17,20 lyase inhibitors |
| WO2003027094A2 (en) | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Substituted 3-pyridyl indoles and indazoles as c17,20 lyase inhibitors |
| RS50504A (sr) | 2001-11-08 | 2007-04-10 | Elan Pharmaceuticals Inc., | Derivati n,n'-supstituisanog-1,3- diamino-2-hidroksipropana |
| DE60304718T2 (de) * | 2002-08-06 | 2007-04-26 | Astrazeneca Ab | Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität |
| PL375532A1 (en) | 2002-08-08 | 2005-11-28 | Smithkline Beecham Corporation | Benzimidazol-1-yl-thiophene compounds for the treatment of cancer |
| EP1534279A4 (en) | 2002-08-14 | 2006-11-08 | Ppd Discovery Inc | INHIBITORS OF PRENYLATION CONTAINING DIMETHYLCYCLOBUTANE, METHODS OF SYNTHESIS AND USE THEREOF |
| AU2003265395A1 (en) | 2002-08-14 | 2004-03-03 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| AR044519A1 (es) | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| US6984652B2 (en) | 2003-09-05 | 2006-01-10 | Warner-Lambert Company Llc | Gyrase inhibitors |
| WO2005074642A2 (en) | 2004-01-30 | 2005-08-18 | Smithkline Beecham Corporation | Chemical compounds |
| CN1989131A (zh) | 2004-03-30 | 2007-06-27 | 希龙公司 | 取代的噻吩衍生物用作抗癌药 |
| JP2008503446A (ja) | 2004-05-06 | 2008-02-07 | プレキシコン，インコーポレーテッド | Ｐｄｅ４ｂ阻害剤及びその使用 |
| GB0423653D0 (en) | 2004-10-25 | 2004-11-24 | Piramed Ltd | Pharmaceutical compounds |
| CN101084194A (zh) | 2004-12-21 | 2007-12-05 | 默克公司 | 有丝分裂驱动蛋白抑制剂 |
| CA2594477C (en) | 2005-01-21 | 2016-07-12 | Astex Therapeutics Limited | Pharmaceutical compounds |
| 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 |
| PT1869049E (pt) | 2005-03-21 | 2009-05-26 | Lilly Co Eli | Compostos de imidazopiridazina |
| GB0508471D0 (en) | 2005-04-26 | 2005-06-01 | Celltech R&D Ltd | Therapeutic agents |
| GB0508472D0 (en) | 2005-04-26 | 2005-06-01 | Glaxo Group Ltd | Compounds |
| WO2007002563A1 (en) | 2005-06-27 | 2007-01-04 | Exelixis, Inc. | Imidazole based lxr modulators |
| 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 |
| CN101374808B (zh) | 2006-01-24 | 2011-05-25 | 伊莱利利公司 | 孕酮受体的吲哚磺酰胺调节剂 |
| US7504513B2 (en) | 2006-02-27 | 2009-03-17 | Hoffman-La Roche Inc. | Thiazolyl-benzimidazoles |
| UA94097C2 (ru) | 2006-03-27 | 2011-04-11 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Пиридил- и пиримидинилзамещенные производной пиррола, тиофена и фурана как ингибиторы киназ |
| RU2439074C2 (ru) | 2006-04-26 | 2012-01-10 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНОЕ ТИЕНО[3,2-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (РI3К) |
| WO2007129044A1 (en) | 2006-05-03 | 2007-11-15 | Astrazeneca Ab | Thiazole derivatives and their use as anti-tumour agents |
| AU2007267986A1 (en) | 2006-05-23 | 2007-12-06 | 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 |
| 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 |
| EP2385050A1 (en) | 2006-08-14 | 2011-11-09 | Schering Corporation | A process for preparing a substituted oxazole |
| US20090093452A1 (en) | 2006-08-24 | 2009-04-09 | Pfizer Inc. | Pyrrole, Thiophene, Furan, Imidazole, Oxazole, and Thiazole Derivatives |
| JP5534811B2 (ja) | 2006-08-24 | 2014-07-02 | アストラゼネカ アクチボラグ | 増殖性疾患の治療に有用なモルホリノピリミジン誘導体 |
| AU2007290359B2 (en) * | 2006-09-01 | 2012-09-20 | Vertex Pharmaceuticals Incorporated | 5- (2-furyl)-1, 3-thiazole derivatives useful as inhibitors of phosphatidylinositol 3-kinase |
| CA2662000C (en) | 2006-09-20 | 2013-01-08 | Eli Lilly And Company | Thiophene pyrazolopyrimidine compounds |
| WO2008068470A1 (en) | 2006-12-04 | 2008-06-12 | Astrazeneca Ab | Antibacterial polycyclic urea compounds |
| 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 |
| AU2008214095B2 (en) | 2007-02-02 | 2014-07-10 | 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 |
| WO2008098105A1 (en) | 2007-02-07 | 2008-08-14 | Smithkline Beecham Corporation | Inhibitors of akt activity |
| NZ598890A (en) | 2007-04-30 | 2013-10-25 | Genentech Inc | Inhibitors of 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 |
| CA2699328A1 (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 |
| RU2506267C2 (ru) | 2008-03-31 | 2014-02-10 | Дженентек, Инк. | Бензопирановые и бензоксепиновые ингибиторы рi3k и их применение |
| GB0805818D0 (en) | 2008-03-31 | 2008-04-30 | Ucb Pharma Sa | Therapeutic agents |
| BRPI0914223A2 (pt) | 2008-06-19 | 2019-09-24 | Millennium Pharm Inc | derivados de tiofeno ou tiazol e seus usos como inibidores de p13k |
| EP2303852A4 (en) * | 2008-06-26 | 2011-12-28 | Glaxosmithkline Llc | ACTIVITY INHIBITORS AKT |
| GB0812309D0 (en) | 2008-07-03 | 2008-08-13 | Ucb Pharma Sa | Therapeutic agents |
| CA2730010A1 (en) | 2008-07-09 | 2010-01-14 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
| CN102171196B (zh) | 2008-08-04 | 2015-03-25 | 默沙东公司 | 用作脂肪酸酰胺水解酶的抑制剂的*唑衍生物 |
| WO2010056320A2 (en) | 2008-11-11 | 2010-05-20 | Tyrogenex, Inc. | Pi3k/mtor kinase inhibitors |
| GB0820819D0 (en) | 2008-11-13 | 2008-12-24 | Sareum Ltd | Pharmaceutical compounds |
| EP2378879A4 (en) | 2008-12-16 | 2012-06-06 | Merck Sharp & Dohme | TRIAZONE DERIVATIVES FOR THE TREATMENT OF MORBUS ALZHEIMER |
| 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 |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| 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 |
| WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MA34797B1 (fr) | 2010-08-11 | 2014-01-02 | Millennium Pharm Inc | Hétéroaryles et leurs utilisations |
| WO2012051410A2 (en) | 2010-10-13 | 2012-04-19 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| UY34539A (es) | 2011-12-23 | 2013-06-28 | Millennium Pharm Inc | Heteroarilos y usos de los mismos |
-
2011
- 2011-08-10 EP EP11816983.8A patent/EP2603216A4/en not_active Withdrawn
- 2011-08-10 US US13/206,671 patent/US8859768B2/en active Active
- 2011-08-10 JP JP2013524201A patent/JP2013533318A/ja active Pending
- 2011-08-10 WO PCT/US2011/047245 patent/WO2012021615A1/en not_active Ceased
- 2011-08-11 AR ARP110102930A patent/AR082666A1/es unknown
- 2011-08-11 TW TW100128763A patent/TW201217362A/zh unknown