JP2016530209A5 - - Google Patents
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- Publication number
- JP2016530209A5 JP2016530209A5 JP2016515446A JP2016515446A JP2016530209A5 JP 2016530209 A5 JP2016530209 A5 JP 2016530209A5 JP 2016515446 A JP2016515446 A JP 2016515446A JP 2016515446 A JP2016515446 A JP 2016515446A JP 2016530209 A5 JP2016530209 A5 JP 2016530209A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- unsubstituted
- alkylene
- nhc
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 33
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 21
- 150000002367 halogens Chemical class 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 17
- 239000012453 solvate Substances 0.000 claims 17
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 12
- 125000004430 oxygen atom Chemical group O* 0.000 claims 10
- 125000004434 sulfur atom Chemical group 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 229910052801 chlorine Inorganic materials 0.000 claims 8
- -1 cyclopropyl-1,1-diyl Chemical group 0.000 claims 8
- 229910052731 fluorine Inorganic materials 0.000 claims 8
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 7
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 6
- 229910052794 bromium Inorganic materials 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000003831 tetrazolyl group Chemical group 0.000 claims 6
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 4
- 229910052740 iodine Inorganic materials 0.000 claims 4
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000002098 pyridazinyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 2
- 229910052805 deuterium Inorganic materials 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 2
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 102100021977 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Human genes 0.000 claims 1
- 108050004000 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Proteins 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004410 intraocular pressure Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361878922P | 2013-09-17 | 2013-09-17 | |
| US61/878,922 | 2013-09-17 | ||
| PCT/US2014/055901 WO2015042053A1 (en) | 2013-09-17 | 2014-09-16 | Vinyl autotaxin inhibitor compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016530209A JP2016530209A (ja) | 2016-09-29 |
| JP2016530209A5 true JP2016530209A5 (enExample) | 2017-10-26 |
Family
ID=52689326
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016515446A Pending JP2016530209A (ja) | 2013-09-17 | 2014-09-16 | ビニルオートタキシン阻害剤化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9714240B2 (enExample) |
| EP (1) | EP3046905A4 (enExample) |
| JP (1) | JP2016530209A (enExample) |
| WO (1) | WO2015042053A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9951026B2 (en) | 2013-09-17 | 2018-04-24 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| US9714240B2 (en) | 2013-09-17 | 2017-07-25 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| EP3049405A4 (en) | 2013-09-26 | 2017-03-08 | Pharmakea Inc. | Autotaxin inhibitor compounds |
| CA2930735A1 (en) | 2013-11-22 | 2015-05-28 | Sabre Therapeutics Llc | Tetracyclic autotaxin inhibitors |
| KR102367876B1 (ko) | 2013-11-22 | 2022-02-24 | 사브레 테라퓨틱스 엘엘씨 | 오토탁신 억제제 화합물 |
| CR20160496A (es) | 2014-04-04 | 2017-01-02 | X-Rx Inc | Inhibidores espirocíclicos sustituidos de la autotaxina |
| EA036337B1 (ru) | 2015-05-27 | 2020-10-28 | Сабре Терапьютикс Ллс | Ингибиторы аутотаксина и их применения |
| CA2988306A1 (en) | 2015-06-05 | 2016-12-08 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of demyelinating diseases |
| WO2018106643A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Heterocyclic azoles for the treatment of demyelinating diseases |
| WO2018106641A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Pyrazoles for the treatment of demyelinating diseases |
| WO2018106646A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Aminotriazoles for the treatment of demyelinating diseases |
| CN107226810B (zh) * | 2017-06-16 | 2020-04-28 | 郑州大学 | 吲哚衍生物及其制备方法和其抗流感病毒作用 |
| PH12019502776A1 (en) | 2017-06-30 | 2020-10-26 | Univ California | Compositions and methods for modulating hair growth |
| US12559490B2 (en) | 2020-06-30 | 2026-02-24 | The Regents Of The University Of California | Compositions and methods for modulating hair growth |
| WO2022006470A1 (en) | 2020-07-01 | 2022-01-06 | Vanderbilt University | Methods of treatment for a kidney disease |
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| AU6910994A (en) * | 1993-05-14 | 1994-12-12 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Methods and compounds for inhibiting cell proliferative disorders characterized by abnormal (abl) activity |
| JP2000336075A (ja) * | 1999-05-26 | 2000-12-05 | Sankyo Co Ltd | アクリロニトリル誘導体 |
| CA2386750A1 (en) | 1999-10-22 | 2001-05-03 | Merck & Co. Inc. | Pharmaceuticals for treating obesity |
| EP1390029B1 (en) | 2001-04-11 | 2009-12-16 | Idenix (Cayman) Limited | Phenylindoles for the treatment of hiv |
| HRPK20040271B3 (en) | 2001-09-27 | 2006-02-28 | F. Hoffmann - La Roche Ag | Indole derivatives as cox ii inhibitors |
| WO2003087087A2 (en) | 2002-04-09 | 2003-10-23 | Astex Technology Limited | Heterocyclic compounds and their use as modulators of p38 map kinase |
| JP4340232B2 (ja) | 2002-08-29 | 2009-10-07 | メルク エンド カムパニー インコーポレーテッド | 抗糖尿病活性を有するインドール類 |
| NZ538031A (en) | 2002-08-29 | 2007-10-26 | Merck & Co Inc | Indoles having anti-diabetic activity |
| CN1787817B (zh) | 2003-05-19 | 2011-09-07 | Irm责任有限公司 | 免疫抑制剂化合物及组合物 |
| ATE396970T1 (de) | 2003-12-23 | 2008-06-15 | Lundbeck & Co As H | 2-(1h-indolylsulfanyl)-benzylaminderivate als ssri |
| WO2006041961A1 (en) | 2004-10-05 | 2006-04-20 | GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTHAND HUMAN SERVICES | Arylthioindole tubulin polymerization inhibitors and methods of treating or preventing cancer using same |
| WO2007134169A2 (en) | 2006-05-10 | 2007-11-22 | Nuada, Llc | Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof |
| US20080319044A1 (en) | 2004-11-01 | 2008-12-25 | Nuada, Llc | Compounds and Methods of Use Thereof |
| US20060270634A1 (en) | 2005-05-06 | 2006-11-30 | Miller Duane D | Acetal phosphate-derived LPA mimics, PPARgamma activators, and autotaxin inhibitors |
| AR054394A1 (es) | 2005-06-17 | 2007-06-20 | Lundbeck & Co As H | Derivados de 2- (1h-indolilsulfanil)-aril amina |
| EP2049520A4 (en) | 2006-08-07 | 2011-01-05 | Ironwood Pharmaceuticals Inc | indole compounds |
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| DE102007047737A1 (de) | 2007-10-05 | 2009-04-30 | Merck Patent Gmbh | Piperidin- und Piperazinderivate |
| US8268891B1 (en) | 2007-11-13 | 2012-09-18 | University Of Memphis Research Foundation | Autotaxin inhibitors |
| US8378100B2 (en) | 2008-01-09 | 2013-02-19 | University Of Virginia Patent Foundation | Phosphonate derivatives as autotaxin inhibitors |
| WO2009151644A2 (en) | 2008-06-13 | 2009-12-17 | Yale University | Small molecule inhibitors of autotaxin methods of use |
| WO2010040080A1 (en) | 2008-10-03 | 2010-04-08 | Abby Louise Parrill-Baker | Mechanism-based inactivators of autotaxin |
| DE102008059578A1 (de) | 2008-11-28 | 2010-06-10 | Merck Patent Gmbh | Benzo-Naphtyridin Verbindungen |
| EA201100879A1 (ru) | 2008-12-01 | 2012-01-30 | Мерк Патент Гмбх | Производные пиридопиримидина в качестве ингибиторов аутотаксина |
| EP2623101B1 (en) | 2009-04-02 | 2021-04-21 | Merck Patent GmbH | Piperidine and piperazine derivatives as autotaxin inhibitors |
| JP5767205B2 (ja) | 2009-04-02 | 2015-08-19 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | オートタキシン阻害剤としての複素環式化合物 |
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| WO2011002918A1 (en) | 2009-06-30 | 2011-01-06 | The University Of Memphis Research Foundation | Novel diverse lead compound autotaxin inhibitors |
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| US8497371B2 (en) | 2009-10-26 | 2013-07-30 | University Of Memphis Research Foundation | Pipemidic acid derivative autotaxin inhibitors |
| EP3138838A1 (en) * | 2010-01-29 | 2017-03-08 | Dana-Farber Cancer Institute, Inc. | Small molecules for the modulation of mcl-1 and methods of modulating cell death, cell division, cell differentiation and methods of treating disorders |
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| US9951026B2 (en) | 2013-09-17 | 2018-04-24 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| US9714240B2 (en) | 2013-09-17 | 2017-07-25 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| EP3049405A4 (en) | 2013-09-26 | 2017-03-08 | Pharmakea Inc. | Autotaxin inhibitor compounds |
| CA2930735A1 (en) | 2013-11-22 | 2015-05-28 | Sabre Therapeutics Llc | Tetracyclic autotaxin inhibitors |
| KR102367876B1 (ko) | 2013-11-22 | 2022-02-24 | 사브레 테라퓨틱스 엘엘씨 | 오토탁신 억제제 화합물 |
| US9051320B1 (en) | 2014-08-18 | 2015-06-09 | Pharmakea, Inc. | Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor |
-
2014
- 2014-09-16 US US15/022,167 patent/US9714240B2/en not_active Expired - Fee Related
- 2014-09-16 EP EP14846301.1A patent/EP3046905A4/en not_active Withdrawn
- 2014-09-16 WO PCT/US2014/055901 patent/WO2015042053A1/en not_active Ceased
- 2014-09-16 JP JP2016515446A patent/JP2016530209A/ja active Pending