JP2008545652A5 - - Google Patents
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- JP2008545652A5 JP2008545652A5 JP2008512402A JP2008512402A JP2008545652A5 JP 2008545652 A5 JP2008545652 A5 JP 2008545652A5 JP 2008512402 A JP2008512402 A JP 2008512402A JP 2008512402 A JP2008512402 A JP 2008512402A JP 2008545652 A5 JP2008545652 A5 JP 2008545652A5
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- optionally substituted
- substituted
- group
- nhr
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 73
- 125000003545 alkoxy group Chemical group 0.000 claims 44
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000004414 alkyl thio group Chemical group 0.000 claims 32
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 239000001257 hydrogen Substances 0.000 claims 32
- 125000001153 fluoro group Chemical group F* 0.000 claims 30
- 229910052757 nitrogen Inorganic materials 0.000 claims 29
- 125000001072 heteroaryl group Chemical group 0.000 claims 26
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 25
- 229910052799 carbon Inorganic materials 0.000 claims 22
- 125000001424 substituent group Chemical group 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 150000002431 hydrogen Chemical class 0.000 claims 19
- 101100240528 Caenorhabditis elegans nhr-23 gene Proteins 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 11
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 101100294106 Caenorhabditis elegans nhr-3 gene Proteins 0.000 claims 10
- 125000003107 substituted aryl group Chemical group 0.000 claims 10
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 8
- -1 monoalkylamino Chemical group 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 150000001345 alkine derivatives Chemical class 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 201000006512 mast cell neoplasm Diseases 0.000 claims 4
- 208000006971 mastocytoma Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 150000001336 alkenes Chemical class 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 206010003571 Astrocytoma Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000010392 Bone Fractures Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 241000282465 Canis Species 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 206010014561 Emphysema Diseases 0.000 claims 2
- 206010014950 Eosinophilia Diseases 0.000 claims 2
- 206010017076 Fracture Diseases 0.000 claims 2
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 2
- 208000037147 Hypercalcaemia Diseases 0.000 claims 2
- 206010020880 Hypertrophy Diseases 0.000 claims 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 208000009905 Neurofibromatoses Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010038540 Renal tubular necrosis Diseases 0.000 claims 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 2
- 206010057644 Testis cancer Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 201000010105 allergic rhinitis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 210000000988 bone and bone Anatomy 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 201000010989 colorectal carcinoma Diseases 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 210000005002 female reproductive tract Anatomy 0.000 claims 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 230000000148 hypercalcaemia Effects 0.000 claims 2
- 208000030915 hypercalcemia disease Diseases 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 201000004933 in situ carcinoma Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 201000006334 interstitial nephritis Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 230000004130 lipolysis Effects 0.000 claims 2
- 208000008585 mastocytosis Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000009401 metastasis Effects 0.000 claims 2
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 230000009826 neoplastic cell growth Effects 0.000 claims 2
- 201000008383 nephritis Diseases 0.000 claims 2
- 201000004931 neurofibromatosis Diseases 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 210000004116 schwann cell Anatomy 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 201000003120 testicular cancer Diseases 0.000 claims 2
- 125000004001 thioalkyl group Chemical group 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 108010058398 Macrophage Colony-Stimulating Factor Receptor Proteins 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68204205P | 2005-05-17 | 2005-05-17 | |
| US68205105P | 2005-05-17 | 2005-05-17 | |
| US68206305P | 2005-05-17 | 2005-05-17 | |
| US69296005P | 2005-06-22 | 2005-06-22 | |
| US69275005P | 2005-06-22 | 2005-06-22 | |
| PCT/US2006/018726 WO2007013896A2 (en) | 2005-05-17 | 2006-05-16 | Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008545652A JP2008545652A (ja) | 2008-12-18 |
| JP2008545652A5 true JP2008545652A5 (OSRAM) | 2009-07-02 |
Family
ID=37683773
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008512402A Pending JP2008545652A (ja) | 2005-05-17 | 2006-05-16 | ｃ−ｋｉｔおよびｃ−ｆｍｓ活性を調節する化合物およびその用途 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7846941B2 (OSRAM) |
| EP (1) | EP1885723A2 (OSRAM) |
| JP (1) | JP2008545652A (OSRAM) |
| KR (1) | KR20080027775A (OSRAM) |
| AU (1) | AU2006272951A1 (OSRAM) |
| BR (1) | BRPI0610066A2 (OSRAM) |
| CA (1) | CA2608733A1 (OSRAM) |
| CR (1) | CR9591A (OSRAM) |
| EC (1) | ECSP077985A (OSRAM) |
| IL (1) | IL187344A0 (OSRAM) |
| MX (1) | MX2007014377A (OSRAM) |
| NO (1) | NO20075992L (OSRAM) |
| NZ (1) | NZ563444A (OSRAM) |
| WO (1) | WO2007013896A2 (OSRAM) |
Families Citing this family (102)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7504509B2 (en) | 2003-12-19 | 2009-03-17 | Plexxikon, Inc. | Compounds and methods for development of Ret modulators |
| US7498342B2 (en) | 2004-06-17 | 2009-03-03 | Plexxikon, Inc. | Compounds modulating c-kit activity |
| WO2006030826A1 (ja) | 2004-09-17 | 2006-03-23 | Eisai R & D Management Co., Ltd. | 医薬組成物 |
| WO2007013896A2 (en) * | 2005-05-17 | 2007-02-01 | Plexxikon, Inc. | Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors |
| TWI473808B (zh) | 2005-06-22 | 2015-02-21 | Plexxikon Inc | 用於激酶調節的化合物及方法及其適應症 |
| EP2281901B1 (en) | 2005-08-02 | 2013-11-27 | Eisai R&D Management Co., Ltd. | Anti-tumour pharmaceutical composition with angiogenesis inhibitors |
| AU2006285673B2 (en) * | 2005-09-01 | 2010-12-02 | Eisai R&D Management Co., Ltd. | Method for preparation of pharmaceutical composition having improved disintegratability |
| US20070208053A1 (en) * | 2006-01-19 | 2007-09-06 | Arnold Lee D | Fused heterobicyclic kinase inhibitors |
| JP5682051B2 (ja) * | 2006-05-18 | 2015-03-11 | ファーマサイクリックス，インク． | 細胞内キナーゼ阻害剤 |
| AU2007252506C1 (en) | 2006-05-18 | 2012-07-19 | Eisai R & D Management Co., Ltd. | Antitumor agent for thyroid cancer |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| PE20121126A1 (es) * | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
| JP2010514695A (ja) * | 2006-12-21 | 2010-05-06 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物および方法およびそのための適応症 |
| WO2008079909A1 (en) * | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
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| US8394795B2 (en) | 2008-02-29 | 2013-03-12 | Array Biopharma Inc. | Pyrazole [3, 4-B] pyridine Raf inhibitors |
| WO2009111278A2 (en) * | 2008-02-29 | 2009-09-11 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
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| CN102066372B (zh) | 2009-08-24 | 2014-09-17 | 苏州爱斯鹏药物研发有限责任公司 | 含脲基的5，6元杂芳双环化合物作为激酶抑制剂 |
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| JP2014513724A (ja) | 2011-05-16 | 2014-06-05 | オーエスアイ・ファーマシューティカルズ，エルエルシー | 融合二環キナーゼ阻害剤 |
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-
2010
- 2010-12-01 US US12/958,376 patent/US20110166174A1/en not_active Abandoned
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