JP2006508051A5 - - Google Patents
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- Publication number
- JP2006508051A5 JP2006508051A5 JP2004531559A JP2004531559A JP2006508051A5 JP 2006508051 A5 JP2006508051 A5 JP 2006508051A5 JP 2004531559 A JP2004531559 A JP 2004531559A JP 2004531559 A JP2004531559 A JP 2004531559A JP 2006508051 A5 JP2006508051 A5 JP 2006508051A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- aryl
- heteroaryl
- cycloalkyl
- 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 200
- 125000001072 heteroaryl group Chemical group 0.000 claims 92
- 125000003118 aryl group Chemical group 0.000 claims 86
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 69
- 125000000623 heterocyclic group Chemical group 0.000 claims 66
- 125000001424 substituent group Chemical group 0.000 claims 66
- 229910052736 halogen Inorganic materials 0.000 claims 48
- 125000005843 halogen group Chemical group 0.000 claims 42
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 40
- 229910052757 nitrogen Inorganic materials 0.000 claims 40
- 229910052717 sulfur Inorganic materials 0.000 claims 38
- 229910052799 carbon Inorganic materials 0.000 claims 34
- 125000005842 heteroatom Chemical group 0.000 claims 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims 28
- 229910052760 oxygen Inorganic materials 0.000 claims 26
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 24
- 125000004432 carbon atom Chemical group C* 0.000 claims 22
- 125000004434 sulfur atom Chemical group 0.000 claims 22
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 22
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 20
- 125000004430 oxygen atom Chemical group O* 0.000 claims 20
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 125000003107 substituted aryl group Chemical group 0.000 claims 18
- 125000003710 aryl alkyl group Chemical group 0.000 claims 16
- 239000003814 drug Substances 0.000 claims 16
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims 15
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 claims 15
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 14
- 230000002452 interceptive effect Effects 0.000 claims 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 229940079593 drug Drugs 0.000 claims 11
- -1 1-imidazolyl Chemical group 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 210000000988 bone and bone Anatomy 0.000 claims 9
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 8
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 229940043355 kinase inhibitor Drugs 0.000 claims 7
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 7
- 125000002877 alkyl aryl group Chemical group 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 125000001589 carboacyl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000003226 mitogen Substances 0.000 claims 6
- 125000002924 primary amino group Chemical class [H]N([H])* 0.000 claims 6
- 102000004169 proteins and genes Human genes 0.000 claims 6
- 108090000623 proteins and genes Proteins 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 5
- 230000011164 ossification Effects 0.000 claims 5
- 238000007634 remodeling Methods 0.000 claims 5
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 4
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 208000020084 Bone disease Diseases 0.000 claims 4
- 206010017076 Fracture Diseases 0.000 claims 4
- 229940122696 MAP kinase inhibitor Drugs 0.000 claims 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical group C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 4
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical group N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000003435 aroyl group Chemical group 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical group C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 4
- 150000001768 cations Chemical class 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 239000000126 substance Substances 0.000 claims 4
- 238000006467 substitution reaction Methods 0.000 claims 4
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 4
- 230000002708 enhancing effect Effects 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 2
- 125000004173 1-benzimidazolyl group Chemical group [H]C1=NC2=C([H])C([H])=C([H])C([H])=C2N1* 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 241000180579 Arca Species 0.000 claims 2
- 208000006386 Bone Resorption Diseases 0.000 claims 2
- 101000628954 Homo sapiens Mitogen-activated protein kinase 12 Proteins 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 102100026932 Mitogen-activated protein kinase 12 Human genes 0.000 claims 2
- 108700015928 Mitogen-activated protein kinase 13 Proteins 0.000 claims 2
- 102000056248 Mitogen-activated protein kinase 13 Human genes 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Chemical group C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 206010049514 Traumatic fracture Diseases 0.000 claims 2
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 230000024279 bone resorption Effects 0.000 claims 2
- 210000001612 chondrocyte Anatomy 0.000 claims 2
- 230000004069 differentiation Effects 0.000 claims 2
- 238000000605 extraction Methods 0.000 claims 2
- 230000001815 facial effect Effects 0.000 claims 2
- 239000003205 fragrance Substances 0.000 claims 2
- 230000004927 fusion Effects 0.000 claims 2
- 125000005343 heterocyclic alkyl group Chemical group 0.000 claims 2
- 125000005956 isoquinolyl group Chemical group 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 230000007774 longterm Effects 0.000 claims 2
- 210000002050 maxilla Anatomy 0.000 claims 2
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical group O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 210000002997 osteoclast Anatomy 0.000 claims 2
- 208000028169 periodontal disease Diseases 0.000 claims 2
- LYKMMUBOEFYJQG-UHFFFAOYSA-N piperoxan Chemical group C1OC2=CC=CC=C2OC1CN1CCCCC1 LYKMMUBOEFYJQG-UHFFFAOYSA-N 0.000 claims 2
- 230000001737 promoting effect Effects 0.000 claims 2
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000004546 quinazolin-4-yl group Chemical group N1=CN=C(C2=CC=CC=C12)* 0.000 claims 2
- 125000005493 quinolyl group Chemical group 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 239000011593 sulfur Chemical group 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 230000010072 bone remodeling Effects 0.000 claims 1
- 210000000845 cartilage Anatomy 0.000 claims 1
- 230000022159 cartilage development Effects 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 210000004373 mandible Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 0 *c(nc(*)[n]1*)c1I Chemical compound *c(nc(*)[n]1*)c1I 0.000 description 3
- SECXISVLQFMRJM-UHFFFAOYSA-N CN(CCC1)C1=O Chemical compound CN(CCC1)C1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 1
- JTPZTKBRUCILQD-UHFFFAOYSA-N CN(CCN1)C1=O Chemical compound CN(CCN1)C1=O JTPZTKBRUCILQD-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40666402P | 2002-08-29 | 2002-08-29 | |
| PCT/US2003/026839 WO2004019873A2 (en) | 2002-08-29 | 2003-08-29 | Methods of promoting osteogenesis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006508051A JP2006508051A (ja) | 2006-03-09 |
| JP2006508051A5 true JP2006508051A5 (https=) | 2007-07-19 |
Family
ID=31978337
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004531559A Pending JP2006508051A (ja) | 2002-08-29 | 2003-08-29 | 骨形成を促進する方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7268139B2 (https=) |
| EP (1) | EP1539121A4 (https=) |
| JP (1) | JP2006508051A (https=) |
| AU (1) | AU2003262911A1 (https=) |
| CA (1) | CA2497240A1 (https=) |
| WO (1) | WO2004019873A2 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1539121A4 (en) * | 2002-08-29 | 2008-08-13 | Scios Inc | METHOD OF REQUESTING OSTEOGENESIS |
| US20090075941A1 (en) * | 2006-04-21 | 2009-03-19 | The Uab Research Foundation | Treating neoplasms |
| US20070269440A1 (en) * | 2006-05-22 | 2007-11-22 | Board Of Trustees Of The University Of Arkansas | Stimulators of osteoblastogenesis and applications of the same |
| US20120276064A1 (en) * | 2011-04-05 | 2012-11-01 | Blau Helen M | Methods and compositions for rejuvenation and expansion of stem cells |
| BR112015022471A2 (pt) * | 2013-03-15 | 2017-08-22 | Theocorp Holding Co Llc | Composições de teobromina úteis para aumentar o ganho de peso do feto e acentuar as propriedades ósseas |
| GB201317609D0 (en) | 2013-10-04 | 2013-11-20 | Cancer Rec Tech Ltd | Inhibitor compounds |
| GB201505658D0 (en) | 2015-04-01 | 2015-05-13 | Cancer Rec Tech Ltd | Inhibitor compounds |
| GB201617103D0 (en) | 2016-10-07 | 2016-11-23 | Cancer Research Technology Limited | Compound |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| WO2019071147A1 (en) | 2017-10-05 | 2019-04-11 | Fulcrum Therapeutics, Inc. | INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| US4619652A (en) | 1982-12-23 | 1986-10-28 | Alza Corporation | Dosage form for use in a body mounted pump |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| US5593992A (en) | 1993-07-16 | 1997-01-14 | Smithkline Beecham Corporation | Compounds |
| FI972970A7 (fi) | 1995-01-12 | 1997-09-11 | Smithkline Beecham Corp | Uusia yhdisteitä |
| IL118544A (en) | 1995-06-07 | 2001-08-08 | Smithkline Beecham Corp | History of imidazole, the process for their preparation and the pharmaceutical preparations containing them |
| ZA97175B (en) * | 1996-01-11 | 1997-11-04 | Smithkline Beecham Corp | Novel substituted imidazole compounds. |
| JP2000507558A (ja) | 1996-03-25 | 2000-06-20 | スミスクライン・ビーチャム・コーポレイション | Ｃｎｓ損傷についての新規な治療 |
| ZA9711092B (en) | 1996-12-11 | 1999-07-22 | Smithkline Beecham Corp | Novel compounds. |
| CA2294057A1 (en) | 1997-06-13 | 1998-12-17 | Smithkline Beecham Corporation | Novel pyrazole and pyrazoline substituted compounds |
| AU8154998A (en) | 1997-06-19 | 1999-01-04 | Smithkline Beecham Corporation | Novel aryloxy substituted pyrimidine imidazole compounds |
| WO1999032121A1 (en) | 1997-12-19 | 1999-07-01 | Smithkline Beecham Corporation | Compounds of heteroaryl substituted imidazole, their pharmaceutical compositions and uses |
| JP3887769B2 (ja) | 1997-12-22 | 2007-02-28 | バイエル コーポレイション | 対称および非対称ジフェニル尿素を用いるｐ３８キナーゼの阻害 |
| DE69836563T2 (de) | 1997-12-22 | 2007-05-16 | Bayer Pharmaceuticals Corp., West Haven | INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN |
| CA2329065A1 (en) | 1998-05-05 | 1999-11-11 | Francisco Xavier Talamas | Pyrazole derivatives as p-38 map kinase inhibitors |
| WO1999061440A1 (en) | 1998-05-26 | 1999-12-02 | Smithkline Beecham Corporation | Novel substituted imidazole compounds |
| JP2002517486A (ja) | 1998-06-12 | 2002-06-18 | 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 | ｐ３８のインヒビター |
| JP2003525201A (ja) | 1998-08-20 | 2003-08-26 | スミスクライン・ビーチャム・コーポレイション | 新規な置換トリアゾール化合物 |
| CA2342251A1 (en) | 1998-08-28 | 2000-03-09 | Scios Inc. | Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase |
| AR023659A1 (es) | 1998-09-18 | 2002-09-04 | Vertex Pharma | Un compuesto inhibidor de p38, una composicion farmaceutica que lo comprende y el uso de dicha composicion en el tratamiento y prevencion de estados patologicos |
| CA2346665A1 (en) | 1998-10-07 | 2000-04-13 | Smithkline Beecham Corporation | Novel treatment for stroke management |
| AU6476599A (en) * | 1998-11-03 | 2000-05-22 | Novartis Ag | Anti-inflammatory 4-phenyl-5-pyrimidinyl-imidazoles |
| AU765492B2 (en) * | 1998-12-25 | 2003-09-18 | Teikoku Hormone Mfg. Co., Ltd. | Aminopyrazole derivatives |
| ATE538794T1 (de) | 1999-01-13 | 2012-01-15 | Bayer Healthcare Llc | Gamma carboxyarylsubstituierte diphenylharnstoffverbindungen als p38 kinasehemmer |
| EP1173254A2 (en) | 1999-04-27 | 2002-01-23 | Smithkline Beecham Plc | Novel treatment of neurotraumatic conditions with a raf inhibitor |
| JP2003500403A (ja) | 1999-05-21 | 2003-01-07 | サイオス，インコーポレーテッド | ｐ３８キナーゼのインヒビターとしてのインドール型誘導体 |
| RU2240995C2 (ru) | 1999-07-16 | 2004-11-27 | Лео Фармасьютикал Продактс Лтд.А/С (Левенс Кемиске Фабрик Продукционсактиесельскаб) | Аминобензофеноны в качестве ингибиторов интерлейкина il-1бета и фактора некроза опухолей tnf-альфа |
| EP1205478A4 (en) | 1999-08-06 | 2004-06-30 | Takeda Chemical Industries Ltd | P38MAP KINASE INHIBITORS |
| TR200201364T2 (tr) | 1999-11-22 | 2002-10-21 | Smithkline Beecham P. L. C. | Yeni bileşikler. |
| MY141144A (en) | 2000-03-02 | 2010-03-15 | Smithkline Beecham Corp | 1, 5-disubstituted-3,4-dihydro-1h-pyrimido 4,5-dipyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases |
| GB0005357D0 (en) | 2000-03-06 | 2000-04-26 | Smithkline Beecham Plc | Compounds |
| ES2218391T3 (es) | 2000-03-06 | 2004-11-16 | Smithkline Beecham Plc | Derivados de imidazol como inhibidores de raf-cinasa. |
| US6565880B2 (en) | 2000-07-24 | 2003-05-20 | Boehringer Ingelheim Pharmaceuticals, Inc. | Oral dosage formulations of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea |
| EP1539121A4 (en) * | 2002-08-29 | 2008-08-13 | Scios Inc | METHOD OF REQUESTING OSTEOGENESIS |
-
2003
- 2003-08-29 EP EP03791848A patent/EP1539121A4/en not_active Withdrawn
- 2003-08-29 US US10/651,934 patent/US7268139B2/en not_active Expired - Lifetime
- 2003-08-29 AU AU2003262911A patent/AU2003262911A1/en not_active Abandoned
- 2003-08-29 WO PCT/US2003/026839 patent/WO2004019873A2/en not_active Ceased
- 2003-08-29 CA CA002497240A patent/CA2497240A1/en not_active Abandoned
- 2003-08-29 JP JP2004531559A patent/JP2006508051A/ja active Pending
-
2007
- 2007-09-11 US US11/853,751 patent/US20080108658A1/en not_active Abandoned
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