JP2005539026A5 - - Google Patents
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- Publication number
- JP2005539026A5 JP2005539026A5 JP2004528450A JP2004528450A JP2005539026A5 JP 2005539026 A5 JP2005539026 A5 JP 2005539026A5 JP 2004528450 A JP2004528450 A JP 2004528450A JP 2004528450 A JP2004528450 A JP 2004528450A JP 2005539026 A5 JP2005539026 A5 JP 2005539026A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- het
- alkoxy
- hydrogen
- methylpyridin
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- BVJXVJYPAZDBEW-UHFFFAOYSA-N (4-ethylpiperazin-1-yl)-[4-[4-[4-(6-methylpyridin-2-yl)-1h-pyrazol-5-yl]pyridin-2-yl]phenyl]methanone Chemical compound C1CN(CC)CCN1C(=O)C1=CC=C(C=2N=CC=C(C=2)C=2C(=CNN=2)C=2N=C(C)C=CC=2)C=C1 BVJXVJYPAZDBEW-UHFFFAOYSA-N 0.000 claims 2
- MMELVGLVJPTMTF-UHFFFAOYSA-N 2-[4-[4-[4-(6-methylpyridin-2-yl)-1h-pyrazol-5-yl]pyridin-2-yl]phenoxy]-1-morpholin-4-ylethanone Chemical compound CC1=CC=CC(C=2C(=NNC=2)C=2C=C(N=CC=2)C=2C=CC(OCC(=O)N3CCOCC3)=CC=2)=N1 MMELVGLVJPTMTF-UHFFFAOYSA-N 0.000 claims 2
- QYFPRQIXLPOKCT-UHFFFAOYSA-N 2-methyl-6-[5-[2-[4-(2-pyrrolidin-1-ylethoxy)phenyl]pyridin-4-yl]-1h-pyrazol-4-yl]pyridine Chemical compound CC1=CC=CC(C=2C(=NNC=2)C=2C=C(N=CC=2)C=2C=CC(OCCN3CCCC3)=CC=2)=N1 QYFPRQIXLPOKCT-UHFFFAOYSA-N 0.000 claims 2
- RPQPZQIYRZCVAF-UHFFFAOYSA-N 4-[4-[4-(6-methylpyridin-2-yl)-1h-pyrazol-5-yl]pyridin-2-yl]-n-(oxan-4-yl)benzamide Chemical compound CC1=CC=CC(C=2C(=NNC=2)C=2C=C(N=CC=2)C=2C=CC(=CC=2)C(=O)NC2CCOCC2)=N1 RPQPZQIYRZCVAF-UHFFFAOYSA-N 0.000 claims 2
- CSTHQMSIDVZWGR-UHFFFAOYSA-N 4-[4-[4-[4-(6-methylpyridin-2-yl)-1h-pyrazol-5-yl]pyridin-2-yl]phenyl]morpholine Chemical compound CC1=CC=CC(C2=C(NN=C2)C=2C=C(N=CC=2)C=2C=CC(=CC=2)N2CCOCC2)=N1 CSTHQMSIDVZWGR-UHFFFAOYSA-N 0.000 claims 2
- OLOUQEIXASCQIR-UHFFFAOYSA-N 4-[[4-[4-[4-(6-methylpyridin-2-yl)-1h-pyrazol-5-yl]pyridin-2-yl]phenyl]methyl]morpholine Chemical compound CC1=CC=CC(C2=C(NN=C2)C=2C=C(N=CC=2)C=2C=CC(CN3CCOCC3)=CC=2)=N1 OLOUQEIXASCQIR-UHFFFAOYSA-N 0.000 claims 2
- 241000711549 Hepacivirus C Species 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000018565 Hemochromatosis Diseases 0.000 claims 1
- 241000700721 Hepatitis B virus Species 0.000 claims 1
- 206010019728 Hepatitis alcoholic Diseases 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 206010023330 Keloid scar Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010027398 Mesenteric fibrosis Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010034665 Peritoneal fibrosis Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000002353 alcoholic hepatitis Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000009251 neurologic dysfunction Effects 0.000 claims 1
- 208000015015 neurological dysfunction Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0217786.3A GB0217786D0 (en) | 2002-07-31 | 2002-07-31 | Compounds |
| PCT/EP2003/008449 WO2004016606A1 (en) | 2002-07-31 | 2003-07-29 | Pyrazole inhibitors of the transforming growth factor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005539026A JP2005539026A (ja) | 2005-12-22 |
| JP2005539026A5 true JP2005539026A5 (https=) | 2006-09-14 |
Family
ID=9941487
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004528450A Pending JP2005539026A (ja) | 2002-07-31 | 2003-07-29 | 形質転換成長因子のピラゾール阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20060058329A1 (https=) |
| EP (1) | EP1554268A1 (https=) |
| JP (1) | JP2005539026A (https=) |
| AU (1) | AU2003255333A1 (https=) |
| GB (1) | GB0217786D0 (https=) |
| WO (1) | WO2004016606A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
| JP2006522130A (ja) * | 2003-04-03 | 2006-09-28 | メルク エンド カムパニー インコーポレーテッド | ナトリウムチャンネル遮断薬としてのビアリール置換ピラゾール |
| US20060063208A1 (en) | 2004-08-02 | 2006-03-23 | Woolf Clifford J | DRG11-responsive (DRAGON) gene and uses thereof |
| TW200639163A (en) * | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| US7968091B2 (en) | 2005-02-16 | 2011-06-28 | The General Hospital Corporation | Methods and compositions to regulate iron metabolism |
| AU2006239929B2 (en) | 2005-04-22 | 2011-11-03 | Alantos Pharmaceuticals Holding, Inc. | Dipeptidyl peptidase-IV inhibitors |
| BRPI0714409A2 (pt) * | 2006-07-14 | 2013-03-12 | Novartis Ag | derivados de pirimidina como inibidores de alk-5 |
| DK2083863T3 (da) | 2006-10-03 | 2015-06-22 | Genzyme Corp | Antistoffer mod tgf-beta til anvendelse til behandling af spædbørn med risiko for udvikling af bronkopulmonal dysplasi |
| WO2008124768A1 (en) | 2007-04-09 | 2008-10-16 | The General Hospital Corporation | Hemojuvelin fusion proteins and uses thereof |
| WO2009089324A1 (en) | 2008-01-08 | 2009-07-16 | Yale University | Compositions and methods for promoting patency of vascular grafts |
| MX2010007604A (es) * | 2008-01-11 | 2010-08-02 | Novartis Ag | Pirimidinas como inhibidores de cinasa. |
| JP6018753B2 (ja) | 2008-11-13 | 2016-11-02 | ザ・ジェネラル・ホスピタル・コーポレイションＴｈｅ Ｇｅｎｅｒａｌ Ｈｏｓｐｉｔａｌ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｍｐ−６の調節によって鉄の恒常性を制御するための方法および組成物 |
| AR081810A1 (es) | 2010-04-07 | 2012-10-24 | Bayer Cropscience Ag | Piridinilpirazoles biciclicos |
| AR088020A1 (es) | 2010-06-30 | 2014-05-07 | Ironwood Pharmaceuticals Inc | Compuestos heterociclicos como estimuladores de sgc |
| EP2637659B1 (en) | 2010-11-09 | 2016-05-18 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| US9446175B2 (en) | 2011-06-03 | 2016-09-20 | Yale University | Compositions and methods for treating and preventing neointimal stenosis |
| US20140308275A1 (en) | 2011-07-27 | 2014-10-16 | Inserm (Institut National De La Sante Et De La Recherche Medicale | Methods for diagnosing and treating myhre syndrome |
| WO2013062544A1 (en) | 2011-10-26 | 2013-05-02 | Seattle Children's Research Institute | Cysteamine in the treatment of fibrotic disease |
| CN106117194A (zh) | 2011-12-27 | 2016-11-16 | 铁木医药有限公司 | 可用作sgc刺激剂的2‑苄基、3‑(嘧啶‑2‑基)取代的吡唑类 |
| CA3007631A1 (en) | 2015-12-11 | 2017-06-15 | Research Institute At Nationwide Children's Hospital | Optimized patient specific non-linear tissue engineered vascular grafts |
| US11583593B2 (en) | 2016-01-14 | 2023-02-21 | Synthis Therapeutics, Inc. | Antibody-ALK5 inhibitor conjugates and their uses |
| JP2022527972A (ja) | 2019-04-02 | 2022-06-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 前悪性病変を有する患者において癌を予測及び予防する方法 |
| AU2021205893A1 (en) * | 2020-01-08 | 2022-06-23 | Synthis Therapeutics, Inc. | ALK5 inhibitor conjugates and uses thereof |
| EP4556478A4 (en) * | 2022-08-08 | 2025-10-22 | Medinno Pharmaceutical Tech Zhuhai Co Ltd | TGF-BETA INHIBITOR COMPOUND AND USE THEREOF |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6514977B1 (en) * | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| PL337020A1 (en) * | 1997-05-22 | 2000-07-31 | Searle & Co | Substituted pyrazoles as kinase p38 inhibitors |
| GB0027987D0 (en) * | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
| WO2002062787A1 (en) * | 2001-02-02 | 2002-08-15 | Glaxo Group Limited | Pyrazoles as tgf inhibitors |
| JP2004521915A (ja) * | 2001-02-02 | 2004-07-22 | グラクソ グループ リミテッド | Ｔｇｆ過剰発現に対するピラゾール誘導体 |
-
2002
- 2002-07-31 GB GBGB0217786.3A patent/GB0217786D0/en not_active Ceased
-
2003
- 2003-07-29 US US10/522,970 patent/US20060058329A1/en not_active Abandoned
- 2003-07-29 EP EP03787752A patent/EP1554268A1/en not_active Withdrawn
- 2003-07-29 WO PCT/EP2003/008449 patent/WO2004016606A1/en not_active Ceased
- 2003-07-29 JP JP2004528450A patent/JP2005539026A/ja active Pending
- 2003-07-29 AU AU2003255333A patent/AU2003255333A1/en not_active Abandoned