JP2014513140A5 - - Google Patents
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- Publication number
- JP2014513140A5 JP2014513140A5 JP2014509512A JP2014509512A JP2014513140A5 JP 2014513140 A5 JP2014513140 A5 JP 2014513140A5 JP 2014509512 A JP2014509512 A JP 2014509512A JP 2014509512 A JP2014509512 A JP 2014509512A JP 2014513140 A5 JP2014513140 A5 JP 2014513140A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- alkoxy
- optionally substituted
- hydrogen
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 84
- 125000003545 alkoxy group Chemical group 0.000 claims 45
- 229910052739 hydrogen Inorganic materials 0.000 claims 35
- 239000001257 hydrogen Substances 0.000 claims 35
- 150000002431 hydrogen Chemical class 0.000 claims 28
- 235000019000 fluorine Nutrition 0.000 claims 27
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims 26
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 26
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 125000001424 substituent group Chemical group 0.000 claims 21
- 229910052731 fluorine Inorganic materials 0.000 claims 20
- 239000011737 fluorine Substances 0.000 claims 20
- 125000001153 fluoro group Chemical group F* 0.000 claims 20
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 17
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 12
- -1 cyano, hydroxyl Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000004043 oxo group Chemical group O=* 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 7
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000003302 alkenyloxy group Chemical group 0.000 claims 4
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000005133 alkynyloxy group Chemical group 0.000 claims 4
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 4
- 150000002148 esters Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- KUTJKNSCJLFSLI-ALCCZGGFSA-N 7-[[2-[(z)-3-(diethylamino)prop-1-enyl]-4-fluorophenyl]sulfonylamino]-4h-pyrrolo[2,1-c][1,4]benzoxazine-6-carboxylic acid Chemical compound CCN(CC)C\C=C/C1=CC(F)=CC=C1S(=O)(=O)NC1=CC=C2N3C=CC=C3COC2=C1C(O)=O KUTJKNSCJLFSLI-ALCCZGGFSA-N 0.000 claims 1
- SLAAQZMWRRKQTK-WAYWQWQTSA-N 8-[[2-[(z)-3-(diethylamino)prop-1-enyl]-4-fluorophenyl]sulfonylamino]-5,6-dihydropyrazolo[5,1-a]isoquinoline-7-carboxylic acid Chemical compound CCN(CC)C\C=C/C1=CC(F)=CC=C1S(=O)(=O)NC1=CC=C(C=2N(N=CC=2)CC2)C2=C1C(O)=O SLAAQZMWRRKQTK-WAYWQWQTSA-N 0.000 claims 1
- HAZPHHLVQDJXPD-WAYWQWQTSA-N 8-[[2-[(z)-3-(diethylamino)prop-1-enyl]-4-fluorophenyl]sulfonylamino]pyrazolo[5,1-a]isoquinoline-7-carboxylic acid Chemical compound CCN(CC)C\C=C/C1=CC(F)=CC=C1S(=O)(=O)NC1=CC=C(C=2N(N=CC=2)C=C2)C2=C1C(O)=O HAZPHHLVQDJXPD-WAYWQWQTSA-N 0.000 claims 1
- 241000282472 Canis lupus familiaris Species 0.000 claims 1
- 241000282326 Felis catus Species 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 102000002933 Thioredoxin Human genes 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000000638 stimulation Effects 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 229940094937 thioredoxin Drugs 0.000 claims 1
- 108060008226 thioredoxin Proteins 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161483275P | 2011-05-06 | 2011-05-06 | |
| US61/483,275 | 2011-05-06 | ||
| PCT/US2012/036793 WO2012154679A1 (en) | 2011-05-06 | 2012-05-07 | Tricyclic pyrazole sulfonamide compounds and methods of making and using same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014513140A JP2014513140A (ja) | 2014-05-29 |
| JP2014513140A5 true JP2014513140A5 (enExample) | 2015-06-25 |
| JP6035327B2 JP6035327B2 (ja) | 2016-11-30 |
Family
ID=46085253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014509512A Expired - Fee Related JP6035327B2 (ja) | 2011-05-06 | 2012-05-07 | 三環式ピラゾールスルホンアミド化合物ならびにその製造および使用方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US9242997B2 (enExample) |
| EP (1) | EP2705035B1 (enExample) |
| JP (1) | JP6035327B2 (enExample) |
| KR (1) | KR20140040739A (enExample) |
| CN (1) | CN103764652B (enExample) |
| AU (1) | AU2012253760B2 (enExample) |
| BR (1) | BR112013028666A2 (enExample) |
| CA (1) | CA2835209A1 (enExample) |
| MX (1) | MX343688B (enExample) |
| WO (1) | WO2012154679A1 (enExample) |
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| WO2010065877A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
| US8642650B2 (en) | 2008-12-04 | 2014-02-04 | Zafgen, Inc. | Methods of treating an overweight or obese subject |
| WO2013055385A2 (en) | 2011-10-03 | 2013-04-18 | Zafgen Corporation | Methods of treating age related disorders |
| CN102639494B (zh) | 2009-10-09 | 2016-11-09 | 扎夫根公司 | 砜化合物及其制备和使用方法 |
| WO2011085198A1 (en) | 2010-01-08 | 2011-07-14 | Zafgen Corporation | Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) |
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| WO2011127304A2 (en) | 2010-04-07 | 2011-10-13 | Zafgen Corporation | Methods of treating an overweight subject |
| WO2012012642A1 (en) | 2010-07-22 | 2012-01-26 | Zafgen Corporation | Tricyclic compounds and methds of making and using same |
| JP5913333B2 (ja) | 2010-10-12 | 2016-04-27 | ザフゲン，インコーポレイテッド | スルホンアミド化合物、およびそれを製造し使用する方法 |
| AU2011336785A1 (en) | 2010-11-29 | 2013-06-20 | Zafgen, Inc | Treatment of obesity using non-daily administration of 6-0-(4 - dimethylaminoethoxy) cinnamoyl fumagillol |
| CN103402989B (zh) | 2011-01-26 | 2016-04-06 | 扎夫根股份有限公司 | 四唑化合物及其制备和使用方法 |
| AU2012225531B2 (en) | 2011-03-08 | 2017-03-30 | Zafgen, Inc | Oxaspiro (2.5) octane derivatives and analogs |
| EP2705035B1 (en) | 2011-05-06 | 2016-12-14 | Zafgen, Inc. | Tricyclic pyrazole sulfonamide compounds and methods of making and using same |
| CN103748094B (zh) | 2011-05-06 | 2016-06-29 | 扎夫根股份有限公司 | 三环磺酰胺化合物及其制备和使用方法 |
| CA2835261C (en) | 2011-05-06 | 2019-06-04 | Zafgen, Inc. | Partially saturated tricyclic compounds and methods of making and using same |
| EP2804866B1 (en) | 2012-01-18 | 2016-11-16 | Zafgen, Inc. | Tricyclic sulfonamide compounds and methods of making and using same |
| EP2804856B1 (en) | 2012-01-18 | 2017-03-15 | Zafgen, Inc. | Tricyclic sulfone compounds and methods of making and using same |
| MX2014013599A (es) | 2012-05-08 | 2015-05-11 | Zafgen Inc | Tratamiento de la obesidad hipotalamica con inhibidores de metap2. |
| US9573918B2 (en) | 2012-05-09 | 2017-02-21 | Zafgen, Inc. | Fumigillol compounds and methods of making and using same |
| EP2925737B1 (en) | 2012-11-05 | 2017-06-14 | Zafgen, Inc. | Tricyclic compounds for use in the treatment and/or control of obesity |
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| EP2917197B1 (en) | 2012-11-05 | 2019-06-05 | Zafgen, Inc. | Tricyclic compounds and methods of making and using same |
| EP2968250B1 (en) | 2013-03-14 | 2019-06-19 | Zafgen, Inc. | Methods of treating renal disease and other disorders |
| CN104592122B (zh) * | 2014-12-09 | 2018-01-23 | 凯莱英医药集团（天津）股份有限公司 | 3‑(4‑甲基‑1h‑咪唑‑1‑基)‑5‑(三氟甲基)苯胺的制备方法 |
| SI3280710T1 (sl) * | 2015-04-09 | 2020-04-30 | Orion Corporation | Postopek za pripravo antagonistov androgenih receptorjev in njihovih intermediatov |
| CN106432255A (zh) | 2015-08-11 | 2017-02-22 | 扎夫根公司 | 烟曲霉素醇螺环化合物和制备和使用其的方法 |
| AR105671A1 (es) | 2015-08-11 | 2017-10-25 | Zafgen Inc | Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso |
| WO2025149636A1 (en) | 2024-01-10 | 2025-07-17 | Baumann Samira | Ultrasound transducer and method for generating ultrasound signals for digital communication via ultrasound trasmission |
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| US20130023513A1 (en) | 2010-01-12 | 2013-01-24 | Hughes Thomas E | Methods and Compositions for Treating Cardiovascular Disorders |
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-
2012
- 2012-05-07 EP EP12721140.7A patent/EP2705035B1/en active Active
- 2012-05-07 KR KR1020137032333A patent/KR20140040739A/ko not_active Withdrawn
- 2012-05-07 CN CN201280033357.9A patent/CN103764652B/zh not_active Expired - Fee Related
- 2012-05-07 AU AU2012253760A patent/AU2012253760B2/en not_active Ceased
- 2012-05-07 CA CA2835209A patent/CA2835209A1/en not_active Abandoned
- 2012-05-07 JP JP2014509512A patent/JP6035327B2/ja not_active Expired - Fee Related
- 2012-05-07 BR BR112013028666A patent/BR112013028666A2/pt active Search and Examination
- 2012-05-07 WO PCT/US2012/036793 patent/WO2012154679A1/en not_active Ceased
- 2012-05-07 MX MX2013012923A patent/MX343688B/es active IP Right Grant
- 2012-05-07 US US14/116,029 patent/US9242997B2/en not_active Expired - Fee Related
-
2015
- 2015-12-14 US US14/968,013 patent/US20160324865A1/en not_active Abandoned
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