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 |
|---|---|---|---|
| US37255310P | 2010-08-11 | 2010-08-11 | |
| US37262810P | 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 |
| 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 |
| WO2010090716A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| TW201217365A (en) | 2010-08-11 | 2012-05-01 | Millennium Pharm Inc | Heteroaryls and uses thereof |
| WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| TW201307309A (zh) | 2010-10-13 | 2013-02-16 | Millennium Pharm Inc | 雜芳基化合物及其用途 |
| SG11201500499TA (en) | 2012-08-10 | 2015-03-30 | Boehringer Ingelheim Int | Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors |
| 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 |
| JP6486954B2 (ja) | 2014-01-29 | 2019-03-20 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂｔｋ阻害剤としてのピラゾール化合物 |
| EP3156405A1 (en) | 2015-10-13 | 2017-04-19 | Boehringer Ingelheim International GmbH | Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide |
| LT3390390T (lt) | 2015-12-16 | 2021-11-25 | Boehringer Ingelheim International Gmbh | Bipirazolilo dariniai, tinkami naudoti autoimuninių ligų gydymui |
| 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 |
| AU6966696A (en) | 1995-10-05 | 1997-04-28 | 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 |
| ES2167882T3 (es) | 1997-04-24 | 2002-05-16 | Dow Agrosciences Llc | 3-(fenil sustituido)-5-(tienil o furil)-1,2,4-triazoles pesticidas. |
| 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 |
| JP2003520233A (ja) | 2000-01-18 | 2003-07-02 | 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 | ジャイレースインヒビターおよびそれらの使用 |
| AU2002338642A1 (en) | 2001-04-13 | 2002-10-28 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| US7074801B1 (en) | 2001-04-26 | 2006-07-11 | Eisai Co., Ltd. | Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof |
| US7405235B2 (en) | 2001-05-04 | 2008-07-29 | Paratek Pharmaceuticals, Inc. | Transcription factor modulating compounds and methods of use thereof |
| ATE325608T1 (de) | 2001-08-13 | 2006-06-15 | Janssen Pharmaceutica Nv | 2,4,5-trisubstituted thiazolyl derivative und deren antiinflammatorische wirkung |
| 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 |
| EP1432706A2 (en) | 2001-09-26 | 2004-06-30 | Bayer Pharmaceuticals Corporation | 3-pyridyl or 4-isoquinolinyl thiazoles as c17,20 lyase inhibitors |
| AU2002359376B2 (en) | 2001-11-08 | 2008-01-10 | Elan Pharmaceuticals, Inc. | N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| DE60304718T2 (de) * | 2002-08-06 | 2007-04-26 | Astrazeneca Ab | Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität |
| BR0313160A (pt) | 2002-08-08 | 2005-07-12 | Smithkline Beecham Corp | Composto, composição farmacêutica, métodos para tratar uma condição e um neoplasmo suscetìvel em um animal em um animal, processo para preparar um composto e uso de um composto |
| WO2004016741A2 (en) | 2002-08-14 | 2004-02-26 | Ppd Discovery, Inc. | Prenylation inhibitors containing dimethyl-cyclobutane and methods of their synthesis and use |
| 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 |
| JP2007519753A (ja) | 2004-01-30 | 2007-07-19 | スミスクライン ビーチャム コーポレーション | 化合物 |
| WO2005095386A1 (en) | 2004-03-30 | 2005-10-13 | Chiron Corporation | Substituted thiophene derivatives as anti-cancer agents |
| 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 |
| CA2589827A1 (en) | 2004-12-21 | 2006-06-29 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| MX2007008781A (es) | 2005-01-21 | 2007-09-11 | Astex Therapeutics Ltd | Compuestos farmaceuticos. |
| 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 |
| 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 |
| BRPI0612287A8 (pt) | 2005-06-27 | 2019-01-22 | Exelixis Inc | composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear |
| JP5222561B2 (ja) | 2005-10-07 | 2013-06-26 | キッセイ薬品工業株式会社 | 含窒素芳香族複素環化合物およびそれを含有する医薬組成物 |
| 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 |
| CA2637933C (en) | 2006-01-24 | 2013-03-12 | Eli Lilly And Company | Indole sulfonamide modulators of progesterone receptors |
| US7504513B2 (en) | 2006-02-27 | 2009-03-17 | Hoffman-La Roche Inc. | Thiazolyl-benzimidazoles |
| BRPI0709680B8 (pt) | 2006-03-27 | 2021-05-25 | Nerviano Medical Sciences Srl | derivados de pirrol, tiofeno e furano substituídos por piridil e piridimil como inibidores de quinase |
| WO2007129161A2 (en) | 2006-04-26 | 2007-11-15 | F. Hoffmann-La Roche Ag | Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor |
| JP2009535386A (ja) | 2006-05-03 | 2009-10-01 | アストラゼネカ アクチボラグ | チアゾール誘導体および抗腫瘍剤としてのその使用 |
| WO2007139816A2 (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 |
| AU2007275221A1 (en) | 2006-07-20 | 2008-01-24 | Allen J. Borchardt | Benzothiophene inhibitors of RHO kinase |
| US20100143499A1 (en) | 2006-07-24 | 2010-06-10 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| BRPI0715051A2 (pt) | 2006-08-14 | 2015-05-19 | Schering Corp | Processo e intermediários para a síntese de derivados de 2-(quinolin-5il)-4,5 dissubstituído-azol |
| WO2008024980A2 (en) | 2006-08-24 | 2008-02-28 | Serenex, Inc. | Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives |
| AU2007287428B2 (en) | 2006-08-24 | 2011-08-11 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| CN101528738A (zh) * | 2006-09-01 | 2009-09-09 | 沃泰克斯药物股份有限公司 | 可用作磷脂酰肌醇3-激酶抑制剂的5-（2-呋喃基）-1，3-噻唑衍生物 |
| JP5184536B2 (ja) | 2006-09-20 | 2013-04-17 | イーライ リリー アンド カンパニー | チオフェンピラゾロピリミジン化合物 |
| RU2469034C2 (ru) | 2006-12-04 | 2012-12-10 | Астразенека Аб | Химические соединения |
| 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 |
| JP5461197B2 (ja) | 2007-02-02 | 2014-04-02 | ベイラー カレッジ オブ メディスン | 代謝障害を処置するための組成物および方法 |
| US8420690B2 (en) | 2007-02-07 | 2013-04-16 | Glaxosmithkline Llc | Inhibitors of Akt activity |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2008134679A1 (en) | 2007-04-30 | 2008-11-06 | 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 |
| JP2010540429A (ja) | 2007-09-24 | 2010-12-24 | アクテリオン ファーマシューティカルズ リミテッド | オレキシン受容体拮抗薬としてのピロリジン類及びピペリジン類 |
| CA2704711C (en) | 2007-09-24 | 2016-07-05 | Genentech, Inc. | Thiazolopyrimidine p13k inhibitor compounds and methods of use |
| 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 |
| MX2010010659A (es) | 2008-03-31 | 2010-10-26 | Genentech Inc | Compuestos de benzopirano y benzoxepina, inhibidores de fosfoinoinositida 3-cinasas y metodos para utilizarlos. |
| ES2491522T3 (es) * | 2008-06-19 | 2014-09-08 | Millennium Pharmaceuticals, Inc. | Derivados de tiofeno o tiazol y su uso como inhibidores de PI3K |
| 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 |
| US8420695B2 (en) | 2008-07-09 | 2013-04-16 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
| AU2009279874B2 (en) | 2008-08-04 | 2015-02-12 | Merck Sharp & Dohme Corp. | Oxazole derivatives useful as inhibitors of FAAH |
| AU2009314544C1 (en) | 2008-11-11 | 2015-11-12 | Xcovery Holding Company Llc | PI3K/mTOR kinase inhibitors |
| GB0820819D0 (en) | 2008-11-13 | 2008-12-24 | Sareum Ltd | Pharmaceutical compounds |
| WO2010071741A1 (en) | 2008-12-16 | 2010-06-24 | Merck Sharp & Dohme Corp. | Triazole derivatives for treatment of alzheimer's disease |
| WO2010080873A1 (en) * | 2009-01-08 | 2010-07-15 | Glaxo Group Limited | Oxazoles as modulators of chemokine receptors |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| WO2010090716A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| 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 |
| TW201217365A (en) | 2010-08-11 | 2012-05-01 | Millennium Pharm Inc | Heteroaryls and uses thereof |
| TW201307309A (zh) | 2010-10-13 | 2013-02-16 | Millennium Pharm Inc | 雜芳基化合物及其用途 |
| TW201332989A (zh) | 2011-12-23 | 2013-08-16 | Millennium Pharm Inc | 雜芳基化合物及其用途 |
-
2011
- 2011-08-10 US US13/206,671 patent/US8859768B2/en active Active
- 2011-08-10 WO PCT/US2011/047245 patent/WO2012021615A1/en not_active Ceased
- 2011-08-10 JP JP2013524201A patent/JP2013533318A/ja active Pending
- 2011-08-10 EP EP11816983.8A patent/EP2603216A4/en not_active Withdrawn
- 2011-08-11 AR ARP110102930A patent/AR082666A1/es unknown
- 2011-08-11 TW TW100128763A patent/TW201217362A/zh unknown