JP2014506565A5 - - Google Patents
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- JP2014506565A5 JP2014506565A5 JP2013550547A JP2013550547A JP2014506565A5 JP 2014506565 A5 JP2014506565 A5 JP 2014506565A5 JP 2013550547 A JP2013550547 A JP 2013550547A JP 2013550547 A JP2013550547 A JP 2013550547A JP 2014506565 A5 JP2014506565 A5 JP 2014506565A5
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- 150000001875 compounds Chemical class 0.000 claims description 29
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 13
- 238000000034 method Methods 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 7
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- -1 methylenedioxy group Chemical group 0.000 claims 5
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000004442 acylamino group Chemical group 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000006823 (C1-C6) acyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 210000004081 cilia Anatomy 0.000 claims 2
- 102000013035 dynein heavy chain Human genes 0.000 claims 2
- 108060002430 dynein heavy chain Proteins 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 230000007441 retrograde transport Effects 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 108090000331 Firefly luciferases Proteins 0.000 description 3
- 108010052090 Renilla Luciferases Proteins 0.000 description 3
- 125000004429 atom Chemical group 0.000 description 3
- 231100000673 dose–response relationship Toxicity 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 2
- 239000006144 Dulbecco’s modified Eagle's medium Substances 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 244000309466 calf Species 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 239000000460 chlorine Substances 0.000 description 2
- 239000003636 conditioned culture medium Substances 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 239000011630 iodine Substances 0.000 description 2
- 229910052740 iodine Inorganic materials 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 238000000465 moulding Methods 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 241000254158 Lampyridae Species 0.000 description 1
- 108060001084 Luciferase Proteins 0.000 description 1
- 239000005089 Luciferase Substances 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- 102000006601 Thymidine Kinase Human genes 0.000 description 1
- 108020004440 Thymidine kinase Proteins 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 239000012069 chiral reagent Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000003701 inert diluent Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 239000007932 molded tablet Substances 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000003325 tomography Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434545P | 2011-01-20 | 2011-01-20 | |
| US61/434,545 | 2011-01-20 | ||
| PCT/US2012/021639 WO2012099916A1 (en) | 2011-01-20 | 2012-01-18 | Quinazolinone inhibitors of dynein |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014506565A JP2014506565A (ja) | 2014-03-17 |
| JP2014506565A5 true JP2014506565A5 (https=) | 2015-03-12 |
Family
ID=45774309
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013550547A Pending JP2014506565A (ja) | 2011-01-20 | 2012-01-18 | ダイニンのキナゾリノン阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9145376B2 (https=) |
| EP (1) | EP2665712A1 (https=) |
| JP (1) | JP2014506565A (https=) |
| AU (1) | AU2012207393A1 (https=) |
| CA (1) | CA2824925A1 (https=) |
| IL (1) | IL227490A0 (https=) |
| WO (1) | WO2012099916A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102015221969A1 (de) * | 2015-11-09 | 2017-05-11 | Technische Universität Dresden | Verfahren zur automatisierten Detektion einer Aktivität von Wirkstoffen in einer Lösung |
| KR102672900B1 (ko) * | 2016-09-01 | 2024-06-10 | (주)아모레퍼시픽 | 2,4-디클로로-a-(3,4-디하이드로-4-옥소-2(1H)-퀴나졸리닐리덴)-β-옥소-벤젠프로판니트릴을 포함하는 멜라닌 증진용 조성물 |
| WO2018213712A1 (en) | 2017-05-18 | 2018-11-22 | Kapoor Tarun M | Pyrazoloquinazolinone antitumor agents |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0995485A (ja) * | 1995-03-16 | 1997-04-08 | Takeda Chem Ind Ltd | 複素環化合物、その製造法および剤 |
| US20050080138A1 (en) * | 1999-09-16 | 2005-04-14 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
| US20050049267A1 (en) * | 2002-03-01 | 2005-03-03 | Pintex Pharmaceuticals, Inc. | Pin1-modulating compounds and methods of use thereof |
| CA2502302A1 (en) * | 2002-11-04 | 2004-05-21 | Nps Pharmaceuticals, Inc. | Quinazolinone compounds as calcilytics |
| EP1913913A3 (en) | 2003-02-12 | 2008-05-28 | The Procter and Gamble Company | Absorbent core for an absorbent article |
| WO2007124171A2 (en) * | 2006-04-20 | 2007-11-01 | Massachusetts Institute Of Technology | Compositions and methods for treating trinucleotide repeat disorders |
| AR062200A1 (es) * | 2006-08-04 | 2008-10-22 | Aeterna Zentaris Gmbh | Derivados de antraceno y su uso para el tratamiento de emfermedades tumorales bengnas y malingnas |
| US20090118421A1 (en) | 2007-11-02 | 2009-05-07 | Momentive Performance Materials Inc. | Copolymer of epoxy compounds and amino silanes |
| US8686102B2 (en) | 2007-11-02 | 2014-04-01 | Momentive Performance Materials Inc. | Textiles treated with copolymers of epoxy compounds and amino silanes having enhanced wet-strength |
| US8119640B2 (en) * | 2008-02-12 | 2012-02-21 | The Board Of Trustees Of The Leland Stanford Junior University | Hedgehog pathway antagonists methods of use |
| CA2746220A1 (en) * | 2008-12-08 | 2010-07-08 | Vm Pharma Llc | Compositions of protein receptor tyrosine kinase inhibitors |
-
2012
- 2012-01-18 WO PCT/US2012/021639 patent/WO2012099916A1/en not_active Ceased
- 2012-01-18 CA CA2824925A patent/CA2824925A1/en not_active Abandoned
- 2012-01-18 AU AU2012207393A patent/AU2012207393A1/en not_active Abandoned
- 2012-01-18 JP JP2013550547A patent/JP2014506565A/ja active Pending
- 2012-01-18 US US13/980,527 patent/US9145376B2/en not_active Expired - Fee Related
- 2012-01-18 EP EP12706722.1A patent/EP2665712A1/en not_active Withdrawn
-
2013
- 2013-07-15 IL IL227490A patent/IL227490A0/en unknown
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