JP2009505960A5 - - Google Patents
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- Publication number
- JP2009505960A5 JP2009505960A5 JP2008524052A JP2008524052A JP2009505960A5 JP 2009505960 A5 JP2009505960 A5 JP 2009505960A5 JP 2008524052 A JP2008524052 A JP 2008524052A JP 2008524052 A JP2008524052 A JP 2008524052A JP 2009505960 A5 JP2009505960 A5 JP 2009505960A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- optionally
- alkyl
- substituted
- alkynyl
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims 74
- 150000001875 compounds Chemical class 0.000 claims 62
- 125000000623 heterocyclic group Chemical group 0.000 claims 60
- 125000003710 aryl alkyl group Chemical group 0.000 claims 54
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 53
- -1 cyano, nitro, guanidino Chemical group 0.000 claims 52
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 52
- 125000000547 substituted alkyl group Chemical group 0.000 claims 52
- 125000001475 halogen functional group Chemical group 0.000 claims 51
- 125000000217 alkyl group Chemical group 0.000 claims 48
- 239000000651 prodrug Substances 0.000 claims 46
- 229940002612 prodrug Drugs 0.000 claims 46
- 150000003839 salts Chemical class 0.000 claims 46
- 239000012453 solvate Substances 0.000 claims 46
- 125000003107 substituted aryl group Chemical group 0.000 claims 44
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 43
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 42
- 125000000304 alkynyl group Chemical group 0.000 claims 39
- 125000004438 haloalkoxy group Chemical group 0.000 claims 37
- 125000001188 haloalkyl group Chemical group 0.000 claims 37
- 125000004404 heteroalkyl group Chemical group 0.000 claims 35
- 125000001424 substituent group Chemical group 0.000 claims 35
- 125000003545 alkoxy group Chemical group 0.000 claims 29
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 24
- 125000003118 aryl group Chemical group 0.000 claims 21
- 125000003342 alkenyl group Chemical group 0.000 claims 20
- 125000003282 alkyl amino group Chemical group 0.000 claims 18
- 125000004663 dialkyl amino group Chemical group 0.000 claims 18
- 125000000539 amino acid group Chemical group 0.000 claims 16
- 229910052757 nitrogen Inorganic materials 0.000 claims 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 13
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 12
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000005907 alkyl ester group Chemical group 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 125000002947 alkylene group Chemical group 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 8
- 229920003169 water-soluble polymer Polymers 0.000 claims 8
- 125000004414 alkyl thio group Chemical group 0.000 claims 6
- 150000001413 amino acids Chemical group 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 125000003831 tetrazolyl group Chemical group 0.000 claims 6
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- UKJLNMAFNRKWGR-UHFFFAOYSA-N cyclohexatrienamine Chemical group NC1=CC=C=C[CH]1 UKJLNMAFNRKWGR-UHFFFAOYSA-N 0.000 claims 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 1
- MQLACMBJVPINKE-UHFFFAOYSA-N 10-[(3-hydroxy-4-methoxyphenyl)methylidene]anthracen-9-one Chemical compound C1=C(O)C(OC)=CC=C1C=C1C2=CC=CC=C2C(=O)C2=CC=CC=C21 MQLACMBJVPINKE-UHFFFAOYSA-N 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 1
- 239000004471 Glycine Substances 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 1
- 239000004473 Threonine Substances 0.000 claims 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 235000009697 arginine Nutrition 0.000 claims 1
- 235000009582 asparagine Nutrition 0.000 claims 1
- 229960001230 asparagine Drugs 0.000 claims 1
- 235000003704 aspartic acid Nutrition 0.000 claims 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 1
- 230000017531 blood circulation Effects 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 1
- 235000004554 glutamine Nutrition 0.000 claims 1
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 1
- 235000014304 histidine Nutrition 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 1
- 229960000310 isoleucine Drugs 0.000 claims 1
- 235000018977 lysine Nutrition 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
- 0 CC(*)c1cc(*)c(*)c(*)c1 Chemical compound CC(*)c1cc(*)c(*)c(*)c1 0.000 description 8
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70223705P | 2005-07-25 | 2005-07-25 | |
| US60/702,237 | 2005-07-25 | ||
| US74941805P | 2005-12-12 | 2005-12-12 | |
| US60/749,418 | 2005-12-12 | ||
| US78048806P | 2006-03-08 | 2006-03-08 | |
| US60/780,488 | 2006-03-08 | ||
| PCT/US2006/028801 WO2007014198A1 (en) | 2005-07-25 | 2006-07-24 | 1, 2, 3 -triazoles inhibitors of tubulin polymerization for the treatment of poliferative disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009505960A JP2009505960A (ja) | 2009-02-12 |
| JP2009505960A5 true JP2009505960A5 (https=) | 2009-09-10 |
| JP5149177B2 JP5149177B2 (ja) | 2013-02-20 |
Family
ID=37478877
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008524052A Expired - Fee Related JP5149177B2 (ja) | 2005-07-25 | 2006-07-24 | 増殖性疾患の治療のための、チューブリンポリマー化の１，２，３−トリアゾール系抑制剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (4) | US7781462B2 (https=) |
| EP (1) | EP1919881B1 (https=) |
| JP (1) | JP5149177B2 (https=) |
| AU (1) | AU2006272652B2 (https=) |
| CA (1) | CA2614919C (https=) |
| ES (1) | ES2408597T3 (https=) |
| TW (1) | TWI462908B (https=) |
| WO (1) | WO2007014198A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5149177B2 (ja) | 2005-07-25 | 2013-02-20 | シンタ ファーマシューティカルズ コーポレーション | 増殖性疾患の治療のための、チューブリンポリマー化の１，２，３−トリアゾール系抑制剤 |
| CN101801983B (zh) * | 2007-08-13 | 2014-01-29 | 辛塔制药公司 | 调控hsp90活性的三唑化合物 |
| US9205086B2 (en) | 2010-04-19 | 2015-12-08 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a Hsp90 inhibitory compounds and a EGFR inhibitor |
| US8927547B2 (en) | 2010-05-21 | 2015-01-06 | Noviga Research Ab | Pyrimidine derivatives |
| WO2012084602A1 (en) * | 2010-12-20 | 2012-06-28 | Sigma-Tau Research Switzerland S.A. | Aryl triazole compounds with antitumoural activity |
| EP2502924A1 (en) | 2011-03-24 | 2012-09-26 | Chemilia AB | Novel pyrimidine derivatives |
| DK2688883T3 (en) | 2011-03-24 | 2016-09-05 | Noviga Res Ab | pyrimidine |
| AU2012332424A1 (en) | 2011-11-02 | 2014-06-05 | Synta Pharmaceuticals Corp. | Combination therapy of Hsp90 inhibitors with platinum-containing agents |
| EP2773345A1 (en) | 2011-11-02 | 2014-09-10 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of hsp90 inhibitors with topoisomerase i inhibitors |
| WO2013074594A1 (en) | 2011-11-14 | 2013-05-23 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitors with braf inhibitors |
| EP2711364A1 (en) | 2012-09-21 | 2014-03-26 | Chemilia AB | 4-(Indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer |
| EP2711365A1 (en) | 2012-09-21 | 2014-03-26 | Chemilia AB | 4-Indazolylamino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer |
| HK1215672A1 (zh) | 2012-12-28 | 2016-09-09 | The Board Of Trustees Of The University Of Arkansas | 用於治療炎症和癌症的吲哚類化合物 |
| WO2014172363A2 (en) | 2013-04-19 | 2014-10-23 | The Board Of Trustees Of The University Of Arkansas | Combretastatin analogs |
| WO2015153635A1 (en) * | 2014-03-31 | 2015-10-08 | Board Of Trustees Of The University Of Arkansas | Disubstituted triazole analogs |
| EP2944635B1 (en) * | 2014-05-15 | 2018-11-28 | Council of Scientific & Industrial Research | Pyrazole linked benzimidazole conjugates and a process for preparation thereof |
| WO2017189893A1 (en) | 2016-04-27 | 2017-11-02 | University Of Puerto Rico | 1,5-disubstituted 1,2,3-triazoles are inhibitors of rac/cdc42 gtpases |
| WO2018144910A1 (en) | 2017-02-02 | 2018-08-09 | Bioventures, Llc | Methods of protecting against neurodegeneration |
| CN109456312B (zh) * | 2018-10-29 | 2021-06-04 | 郑州大学 | 1,2,3-三氮唑类微管蛋白聚合抑制剂其合成方法和应用 |
| US11894884B2 (en) | 2019-09-25 | 2024-02-06 | Alarm.Com Incorporated | Modular electrical grid communications platform |
| AU2023273729A1 (en) * | 2022-05-20 | 2024-12-05 | University Of Puerto Rico | 1,4,5-trisubstituted-1,2,3-triazoles and uses thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0027987D0 (en) * | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
| JP2004532234A (ja) | 2001-04-27 | 2004-10-21 | 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 | トリアゾール由来キナーゼインヒビターおよびその使用 |
| CN100509790C (zh) | 2002-06-29 | 2009-07-08 | 赞塔里斯有限公司 | 芳基羰基哌嗪和杂芳基羰基哌嗪及其治疗良性和恶性肿瘤疾病的用途 |
| CA2497971A1 (en) | 2002-09-18 | 2004-04-01 | Pfizer Products Inc. | Triazole derivatives as transforming growth factor (tgf) inhibitors |
| GB0315111D0 (en) * | 2003-06-27 | 2003-07-30 | Cancer Rec Tech Ltd | Substituted 5-membered ring compounds and their use |
| ITRM20030355A1 (it) * | 2003-07-18 | 2005-01-19 | Sigma Tau Ind Farmaceuti | Composti ad attivita' citotossica derivati della combretastatina. |
| JP5149177B2 (ja) | 2005-07-25 | 2013-02-20 | シンタ ファーマシューティカルズ コーポレーション | 増殖性疾患の治療のための、チューブリンポリマー化の１，２，３−トリアゾール系抑制剤 |
-
2006
- 2006-07-24 JP JP2008524052A patent/JP5149177B2/ja not_active Expired - Fee Related
- 2006-07-24 WO PCT/US2006/028801 patent/WO2007014198A1/en not_active Ceased
- 2006-07-24 CA CA2614919A patent/CA2614919C/en not_active Expired - Fee Related
- 2006-07-24 ES ES06788396T patent/ES2408597T3/es active Active
- 2006-07-24 AU AU2006272652A patent/AU2006272652B2/en not_active Ceased
- 2006-07-24 US US11/492,692 patent/US7781462B2/en not_active Expired - Fee Related
- 2006-07-24 EP EP06788396.7A patent/EP1919881B1/en active Active
- 2006-07-25 TW TW095127101A patent/TWI462908B/zh not_active IP Right Cessation
-
2010
- 2010-04-27 US US12/768,164 patent/US20100279410A1/en not_active Abandoned
-
2011
- 2011-10-04 US US13/252,423 patent/US8501790B2/en not_active Expired - Fee Related
-
2013
- 2013-08-01 US US13/956,534 patent/US9175022B2/en not_active Expired - Fee Related
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