JP2016530210A5 - - Google Patents
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- Publication number
- JP2016530210A5 JP2016530210A5 JP2016515449A JP2016515449A JP2016530210A5 JP 2016530210 A5 JP2016530210 A5 JP 2016530210A5 JP 2016515449 A JP2016515449 A JP 2016515449A JP 2016515449 A JP2016515449 A JP 2016515449A JP 2016530210 A5 JP2016530210 A5 JP 2016530210A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- unsubstituted
- pharmaceutically acceptable
- solvate
- 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
Links
- 150000003839 salts Chemical class 0.000 claims 17
- 239000012453 solvate Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- -1 cyclopropyl-1,1-diyl Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000004430 oxygen atom Chemical group O* 0.000 claims 8
- 125000004434 sulfur atom Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 5
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- 125000003831 tetrazolyl group Chemical group 0.000 claims 5
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000004306 triazinyl group Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000001786 isothiazolyl group Chemical group 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 2
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 2
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 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
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl 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
- 229910052740 iodine Inorganic materials 0.000 claims 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 2
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 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
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 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
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 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
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361878945P | 2013-09-17 | 2013-09-17 | |
| US61/878,945 | 2013-09-17 | ||
| PCT/US2014/055899 WO2015042052A1 (en) | 2013-09-17 | 2014-09-16 | Heterocyclic vinyl autotaxin inhibitor compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016530210A JP2016530210A (ja) | 2016-09-29 |
| JP2016530210A5 true JP2016530210A5 (enExample) | 2017-10-26 |
Family
ID=52689325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016515449A Pending JP2016530210A (ja) | 2013-09-17 | 2014-09-16 | ヘテロ環式ビニルオートタキシン阻害剤化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9951026B2 (enExample) |
| EP (1) | EP3046909A4 (enExample) |
| JP (1) | JP2016530210A (enExample) |
| WO (1) | WO2015042052A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9714240B2 (en) | 2013-09-17 | 2017-07-25 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| EP3046909A4 (en) | 2013-09-17 | 2017-03-29 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| EP3049405A4 (en) | 2013-09-26 | 2017-03-08 | Pharmakea Inc. | Autotaxin inhibitor compounds |
| EP3071561B1 (en) | 2013-11-22 | 2021-03-24 | Sabre Therapeutics LLC | Autotaxin inhibitor compounds |
| US9926318B2 (en) | 2013-11-22 | 2018-03-27 | Pharmakea, Inc. | Tetracyclic autotaxin inhibitors |
| CU24442B1 (es) | 2014-04-04 | 2019-09-04 | X Rx Inc | Derivados de n-(1-(espirocíclico)oxo) amida sustituidos como inhibidores de autotaxina |
| CA2986759C (en) | 2015-05-27 | 2025-06-17 | Sabre Therapeutics Llc | AUTOTAXIN INHIBITORS AND THEIR USES |
| AU2016270373A1 (en) | 2015-06-05 | 2018-01-04 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of demyelinating diseases |
| CN105968049A (zh) * | 2016-04-08 | 2016-09-28 | 深圳市茵诺圣生物科技有限公司 | 一种制备1-(2,6-二氯苄基-3-（吡咯烷-1-甲基）-6-氨基吲唑的方法 |
| 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 |
| WO2018106643A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Heterocyclic azoles for the treatment of demyelinating diseases |
| EP3584241B1 (en) | 2017-02-14 | 2023-04-26 | FUJIFILM Corporation | Method for producing indazole compound, and indazole compound |
| US11166953B2 (en) | 2017-04-17 | 2021-11-09 | Yale University | Compounds, compositions and methods of treating or preventing acute lung injury |
| JP2023502252A (ja) * | 2019-11-20 | 2023-01-23 | イエール ユニバーシティ | 虚血再灌流傷害および／または肺傷害を処置するための化合物、組成物および方法 |
| CN111333580B (zh) * | 2019-12-17 | 2021-09-17 | 温州医科大学 | 一种化合物c18、其制备方法及其在制备抗肺癌药物中的应用 |
| WO2022006470A1 (en) | 2020-07-01 | 2022-01-06 | Vanderbilt University | Methods of treatment for a kidney disease |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| JP2024502337A (ja) | 2021-01-05 | 2024-01-18 | ザイダス ライフサイエンシズ リミティド | オートタキシンの新規阻害剤 |
| CN120882698A (zh) * | 2023-03-31 | 2025-10-31 | 株式会社Lg化学 | 作为自趋化素抑制剂的新型苯并咪唑酮衍生物化合物 |
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| US4271263A (en) | 1980-05-15 | 1981-06-02 | Minnesota Mining And Manufacturing Company | Thermally developable photosensitive compositions containing acutance agents |
| JP2000336075A (ja) | 1999-05-26 | 2000-12-05 | Sankyo Co Ltd | アクリロニトリル誘導体 |
| AU1215701A (en) | 1999-10-22 | 2001-05-08 | Merck & Co., Inc. | Pharmaceuticals for treating obesity |
| US6710068B2 (en) | 2001-04-11 | 2004-03-23 | Idenix Pharmaceuticals, Inc. | 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 |
| CN100457730C (zh) | 2002-08-29 | 2009-02-04 | 默克公司 | 具有抗糖尿病活性的吲哚化合物 |
| EP1546142A4 (en) | 2002-08-29 | 2007-10-17 | Merck & Co Inc | INDOLES HAVING ANTIDIABETIC EFFECT |
| MXPA05012459A (es) | 2003-05-19 | 2006-02-22 | Irm Llc | Compuestos y composiciones inmunosupresoras. |
| PL1701940T3 (pl) | 2003-12-23 | 2008-11-28 | H Lundbeck As | Pochodne 2-(1H-indolilosulfanylo)benzyloaminy jako 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 |
| US20080319044A1 (en) | 2004-11-01 | 2008-12-25 | Nuada, Llc | Compounds and Methods of Use Thereof |
| WO2007134169A2 (en) | 2006-05-10 | 2007-11-22 | Nuada, Llc | Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof 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 |
| SG176477A1 (en) | 2006-08-07 | 2011-12-29 | Ironwood Pharmaceuticals Inc | Indole compounds |
| PE20080668A1 (es) | 2006-08-30 | 2008-07-17 | Novartis Ag | Compuestos heterociclicos como inhibidores de la cinasa-2 de proteina activada por cinasa de proteina activada por mitogeno |
| US8586619B2 (en) | 2007-03-12 | 2013-11-19 | Vm Therapeutics Llc | Agents of calcium ion channel modulators |
| US20090118503A1 (en) | 2007-06-20 | 2009-05-07 | Kevin Sprott | Faah inhibitors |
| 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 |
| US8022239B2 (en) | 2008-10-03 | 2011-09-20 | The University Of Memphis Research Foundation | Mechanism-based inactivators of autotaxin |
| DE102008059578A1 (de) | 2008-11-28 | 2010-06-10 | Merck Patent Gmbh | Benzo-Naphtyridin Verbindungen |
| CN102216299B (zh) * | 2008-12-01 | 2015-02-11 | 默克专利有限公司 | 作为自体毒素抑制剂的2,5-二氨基取代的吡啶并[4,3-d]嘧啶化合物 |
| MX2011010218A (es) | 2009-04-02 | 2011-10-10 | Merck Patent Gmbh | Inhibidores de autotaxina. |
| EA201101399A1 (ru) | 2009-04-02 | 2012-08-30 | Мерк Патент Гмбх | Гетероциклические соединения в качестве ингибиторов аутотаксина |
| CN102369186B (zh) | 2009-04-02 | 2014-07-09 | 默克专利有限公司 | 作为自分泌运动因子抑制剂的哌啶和哌嗪衍生物 |
| EP2266562A1 (en) | 2009-06-23 | 2010-12-29 | Centre National de la Recherche Scientifique | Use of derivatives of indoles for the treatment of cancer |
| WO2011002918A1 (en) | 2009-06-30 | 2011-01-06 | The University Of Memphis Research Foundation | Novel diverse lead compound autotaxin inhibitors |
| DE102009033392A1 (de) | 2009-07-16 | 2011-01-20 | Merck Patent Gmbh | Heterocyclische Verbindungen als Autotaxin-Inhibitoren II |
| DE102009049211A1 (de) | 2009-10-13 | 2011-04-28 | Merck Patent Gmbh | Sulfoxide |
| CN102574843B (zh) | 2009-10-22 | 2015-06-17 | 法博太科制药有限公司 | 抗纤维化剂的稠环类似物 |
| US8497371B2 (en) | 2009-10-26 | 2013-07-30 | University Of Memphis Research Foundation | Pipemidic acid derivative autotaxin inhibitors |
| WO2011053597A1 (en) | 2009-10-26 | 2011-05-05 | The University Of Memphis Research Foundation | Pipemidic acid derivative autotaxin inhibitors |
| CA2787784A1 (en) | 2010-01-29 | 2011-08-04 | 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 |
| AU2011232058B2 (en) | 2010-03-26 | 2016-09-08 | Merck Patent Gmbh | Benzonaphthyridinamines as autotaxin inhibitors |
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| EP2651925A4 (en) | 2010-12-15 | 2014-06-18 | Abbvie Inc | ANTI-VIRAL COMPOUNDS |
| WO2012100018A1 (en) | 2011-01-20 | 2012-07-26 | University Of Tennessee Research Foundation | Inhibitors of autotaxin |
| EP2678050B1 (en) | 2011-02-24 | 2020-10-14 | Emory University | Noggin blocking compositions for ossification and methods related thereto |
| CN103502249A (zh) | 2011-05-17 | 2014-01-08 | 普林斯匹亚生物制药公司 | 作为酪氨酸激酶抑制剂的氮杂吲哚衍生物 |
| EP2714680B1 (en) * | 2011-05-27 | 2015-11-25 | Amira Pharmaceuticals, Inc. | Heterocyclic autotaxin inhibitors and uses thereof |
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| US9630945B2 (en) | 2012-12-19 | 2017-04-25 | Novartis Ag | Autotaxin inhibitors |
| US9409895B2 (en) | 2012-12-19 | 2016-08-09 | Novartis Ag | Autotaxin inhibitors |
| EP3046909A4 (en) | 2013-09-17 | 2017-03-29 | 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 |
| EP3071561B1 (en) | 2013-11-22 | 2021-03-24 | Sabre Therapeutics LLC | Autotaxin inhibitor compounds |
| US9926318B2 (en) | 2013-11-22 | 2018-03-27 | Pharmakea, Inc. | Tetracyclic autotaxin inhibitors |
| 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 EP EP14845959.7A patent/EP3046909A4/en not_active Withdrawn
- 2014-09-16 US US15/022,180 patent/US9951026B2/en active Active
- 2014-09-16 JP JP2016515449A patent/JP2016530210A/ja active Pending
- 2014-09-16 WO PCT/US2014/055899 patent/WO2015042052A1/en not_active Ceased
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