JP2015531764A5 - - Google Patents
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- Publication number
- JP2015531764A5 JP2015531764A5 JP2015527656A JP2015527656A JP2015531764A5 JP 2015531764 A5 JP2015531764 A5 JP 2015531764A5 JP 2015527656 A JP2015527656 A JP 2015527656A JP 2015527656 A JP2015527656 A JP 2015527656A JP 2015531764 A5 JP2015531764 A5 JP 2015531764A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- cycloalkyl
- pharmaceutical composition
- halo
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 44
- -1 CO 2 R Chemical group 0.000 claims description 30
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 22
- 125000005843 halogen group Chemical group 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 15
- 125000006763 (C3-C9) cycloalkyl group Chemical group 0.000 claims description 14
- 125000000623 heterocyclic group Chemical group 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 125000004122 cyclic group Chemical group 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 10
- 208000002193 Pain Diseases 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 7
- 102000048260 kappa Opioid Receptors Human genes 0.000 claims description 5
- 108020001588 κ-opioid receptors Proteins 0.000 claims description 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 125000002619 bicyclic group Chemical group 0.000 claims description 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 4
- 208000018459 dissociative disease Diseases 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 208000004880 Polyuria Diseases 0.000 claims description 3
- 230000035619 diuresis Effects 0.000 claims description 3
- 230000001939 inductive effect Effects 0.000 claims description 3
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical group C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 claims description 2
- 125000006719 (C6-C10) aryl (C1-C6) alkyl group Chemical group 0.000 claims description 2
- 125000004920 4-methyl-2-pentyl group Chemical group CC(CC(C)*)C 0.000 claims description 2
- 208000007848 Alcoholism Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims description 2
- 206010012335 Dependence Diseases 0.000 claims description 2
- 208000019022 Mood disease Diseases 0.000 claims description 2
- 208000004550 Postoperative Pain Diseases 0.000 claims description 2
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims description 2
- 201000007930 alcohol dependence Diseases 0.000 claims description 2
- 230000036506 anxiety Effects 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 208000010877 cognitive disease Diseases 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 2
- 210000000987 immune system Anatomy 0.000 claims description 2
- 230000004112 neuroprotection Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims description 2
- 208000009935 visceral pain Diseases 0.000 claims description 2
- 238000000034 method Methods 0.000 description 13
- 230000009286 beneficial effect Effects 0.000 description 6
- 0 [*-]C1CCCCC1 Chemical compound [*-]C1CCCCC1 0.000 description 2
- 208000017194 Affective disease Diseases 0.000 description 1
- JALJNBDHFVMMOD-UHFFFAOYSA-N C/C(/O)=N/C(c(c(N(CC1)CCC1NC1CCCCC1)nc1c2)cc1cc(C)c2F)N Chemical compound C/C(/O)=N/C(c(c(N(CC1)CCC1NC1CCCCC1)nc1c2)cc1cc(C)c2F)N JALJNBDHFVMMOD-UHFFFAOYSA-N 0.000 description 1
- HROAKQVAEIYWKP-UHFFFAOYSA-N CCC(CCNC1Nc2c(C)cc(C)cc2C=C1C(N)N=O)NC1CCOCC1 Chemical compound CCC(CCNC1Nc2c(C)cc(C)cc2C=C1C(N)N=O)NC1CCOCC1 HROAKQVAEIYWKP-UHFFFAOYSA-N 0.000 description 1
- QEKSAVYVMONYCZ-UHFFFAOYSA-N CCC(CCNC1Nc2cc(F)c(C)cc2C=C1/C(/O)=N/C(C)N)NCC(C)C Chemical compound CCC(CCNC1Nc2cc(F)c(C)cc2C=C1/C(/O)=N/C(C)N)NCC(C)C QEKSAVYVMONYCZ-UHFFFAOYSA-N 0.000 description 1
- CUQCWFSZDAYSHU-UHFFFAOYSA-N CCC(CCNc1ncc(C)cc1-c1ccc(C)[o]1)NC1CCCCC1 Chemical compound CCC(CCNc1ncc(C)cc1-c1ccc(C)[o]1)NC1CCCCC1 CUQCWFSZDAYSHU-UHFFFAOYSA-N 0.000 description 1
- HTILIDJMVWOKSZ-IRQNMHNUSA-N CCC([C@H](CNC1Nc2ccc(C)cc2C=C1/C(/O)=N/[IH]C)OC)NC1CCOCC1 Chemical compound CCC([C@H](CNC1Nc2ccc(C)cc2C=C1/C(/O)=N/[IH]C)OC)NC1CCOCC1 HTILIDJMVWOKSZ-IRQNMHNUSA-N 0.000 description 1
- MVTAUFJNKCAHGP-UHFFFAOYSA-N CCCCCNC1Nc2c(C)cc(C)cc2C=C1C1=NC(C)O1 Chemical compound CCCCCNC1Nc2c(C)cc(C)cc2C=C1C1=NC(C)O1 MVTAUFJNKCAHGP-UHFFFAOYSA-N 0.000 description 1
- DDHFVVYQXZCWAB-UHFFFAOYSA-O CCCCCNC1[NH2+]C=C(C)C=C1C(OC(C)C)=O Chemical compound CCCCCNC1[NH2+]C=C(C)C=C1C(OC(C)C)=O DDHFVVYQXZCWAB-UHFFFAOYSA-O 0.000 description 1
- DZBFTABEDAVECA-UHFFFAOYSA-O CCN=C(C1=Cc2cc(C)cc(C)c2[NH2+]C1NCCC(C(C)CC(C)C)N)N=O Chemical compound CCN=C(C1=Cc2cc(C)cc(C)c2[NH2+]C1NCCC(C(C)CC(C)C)N)N=O DZBFTABEDAVECA-UHFFFAOYSA-O 0.000 description 1
- WSTIPZHCNJPTAR-OSZJVERNSA-N CC[C@H]([C@H](CNc1nc2cc(F)c(C)cc2cc1/C(/O)=N/C(C)N)OC)NC1CCCCC1 Chemical compound CC[C@H]([C@H](CNc1nc2cc(F)c(C)cc2cc1/C(/O)=N/C(C)N)OC)NC1CCCCC1 WSTIPZHCNJPTAR-OSZJVERNSA-N 0.000 description 1
- FUVVKBPFPFMPLW-BVAGGSTKSA-N CC[C@H]([C@H](CNc1nc2ccc(C)cc2cc1-c1ccc(C)[o]1)OC)NC1CCCCC1 Chemical compound CC[C@H]([C@H](CNc1nc2ccc(C)cc2cc1-c1ccc(C)[o]1)OC)NC1CCCCC1 FUVVKBPFPFMPLW-BVAGGSTKSA-N 0.000 description 1
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261683861P | 2012-08-16 | 2012-08-16 | |
| US61/683,861 | 2012-08-16 | ||
| PCT/US2013/055313 WO2014028829A1 (en) | 2012-08-16 | 2013-08-16 | Novel kappa opioid ligands |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017228495A Division JP2018058873A (ja) | 2012-08-16 | 2017-11-29 | 新規カッパオピオイドリガンド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015531764A JP2015531764A (ja) | 2015-11-05 |
| JP2015531764A5 true JP2015531764A5 (enExample) | 2016-07-28 |
| JP6254163B2 JP6254163B2 (ja) | 2017-12-27 |
Family
ID=50101521
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015527656A Active JP6254163B2 (ja) | 2012-08-16 | 2013-08-16 | 新規カッパオピオイドリガンド |
| JP2017228495A Pending JP2018058873A (ja) | 2012-08-16 | 2017-11-29 | 新規カッパオピオイドリガンド |
| JP2020010476A Pending JP2020090518A (ja) | 2012-08-16 | 2020-01-27 | 新規カッパオピオイドリガンド |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017228495A Pending JP2018058873A (ja) | 2012-08-16 | 2017-11-29 | 新規カッパオピオイドリガンド |
| JP2020010476A Pending JP2020090518A (ja) | 2012-08-16 | 2020-01-27 | 新規カッパオピオイドリガンド |
Country Status (8)
| Country | Link |
|---|---|
| US (4) | US9682966B2 (enExample) |
| EP (2) | EP2884978B1 (enExample) |
| JP (3) | JP6254163B2 (enExample) |
| AU (3) | AU2013302497A1 (enExample) |
| CA (1) | CA2882132C (enExample) |
| DK (1) | DK2884978T3 (enExample) |
| ES (1) | ES2750640T3 (enExample) |
| WO (1) | WO2014028829A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2750640T3 (es) | 2012-08-16 | 2020-03-26 | Scripps Research Inst | Ligandos opioides kappa novedosos |
| US10982041B2 (en) * | 2016-02-25 | 2021-04-20 | Swancor Advanced Materials Co., Ltd. | Epoxy resin oligomer |
| EA202092441A1 (ru) | 2016-06-07 | 2021-05-21 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| WO2018170492A1 (en) * | 2017-03-17 | 2018-09-20 | The Scripps Research Institute | Kappa opioid receptor antagonists and products and methods related thereto |
| US10988466B2 (en) | 2017-03-23 | 2021-04-27 | Jacobio Pharmaceuticals Co., Ltd. | Heterocyclic derivatives useful as SHP2 inhibitors |
| WO2019000238A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| WO2019113419A1 (en) * | 2017-12-08 | 2019-06-13 | The Rockefeller University | Pyrano[3,4-b]pyrazine kappa opioid receptor ligands for treating addiction, pruritus, pain, and inflammation |
| US20210393623A1 (en) | 2018-09-26 | 2021-12-23 | Jacobio Pharmaceuticals Co., Ltd. | Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors |
| IL322808A (en) * | 2023-02-17 | 2025-10-01 | Scripps Research Inst | Quinoline derivatives used as kappa-opioid receptor agonists |
| WO2024216061A1 (en) | 2023-04-13 | 2024-10-17 | Neumora Therapeutics, Inc. | Methods of treating depression and anhedonia |
| WO2024216046A1 (en) | 2023-04-13 | 2024-10-17 | Neumora Therapeutics, Inc. | Methods of treating anhedonia |
| WO2025042657A1 (en) * | 2023-08-18 | 2025-02-27 | The Scripps Research Institute | Kappa-opioid receptor antagonists |
| WO2025051204A1 (zh) * | 2023-09-05 | 2025-03-13 | 海思科医药集团股份有限公司 | 一种kor拮抗剂及其在医药上的应用 |
| WO2025250535A1 (en) | 2024-05-28 | 2025-12-04 | Neumora Therapeutics, Inc. | Methods of treating depression and anhedonia |
| WO2025257758A1 (en) | 2024-06-11 | 2025-12-18 | Assia Chemical Industries Ltd. | Solid state forms of navacaprant |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4014171A1 (de) * | 1990-05-03 | 1991-11-07 | Basf Ag | Cyanochinolinverbindungen |
| ES2121988T3 (es) * | 1992-01-23 | 1998-12-16 | Toray Industries | Derivado de morfinano y uso medicinal. |
| WO1999042461A1 (en) | 1998-02-23 | 1999-08-26 | Warner-Lambert Company | Substituted quinoxaline derivatives as interleukin-8 receptor antagonists |
| DE59914996D1 (en) * | 1998-04-20 | 2009-05-14 | Abbott Gmbh & Co Kg | Heterocyclisch substituierte amide als calpainhemmer |
| US6284769B1 (en) * | 1999-12-03 | 2001-09-04 | The Board Of Trustees Of The University Of Illinois | Nonpeptide kappa opioid receptor antagonists |
| US7381721B2 (en) * | 2003-03-17 | 2008-06-03 | Adolor Corporation | Substituted piperidine compounds |
| WO2005028480A2 (en) * | 2003-09-03 | 2005-03-31 | Neurogen Corporation | 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds |
| US7399765B2 (en) | 2003-09-19 | 2008-07-15 | Abbott Laboratories | Substituted diazabicycloalkane derivatives |
| WO2005028438A1 (ja) * | 2003-09-22 | 2005-03-31 | Banyu Pharmaceutical Co., Ltd. | 新規ピペリジン誘導体 |
| ATE533745T1 (de) * | 2004-03-17 | 2011-12-15 | Pfizer Prod Inc | Neue benzyl(iden)-lactam-derivate |
| DK1812440T3 (da) * | 2004-11-04 | 2011-01-31 | Vertex Pharma | Pyrazolo[1,5-a]pyrimidiner, der kan anvendes som inhibistorer af proteinkinaser |
| GB0510204D0 (en) * | 2005-05-19 | 2005-06-22 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| EP2388258A1 (de) | 2005-10-19 | 2011-11-23 | Grünenthal GmbH | Neue Vanilloidrezeptor-Liganden und ihre Verwendung zur Herstellung von Arzneimitteln |
| EP1940406A4 (en) * | 2005-10-21 | 2009-11-18 | Merck & Co Inc | POTASSIUM CHANNEL INHIBITORS |
| JP2010509392A (ja) * | 2006-11-13 | 2010-03-25 | ファイザー・プロダクツ・インク | ジアリール、ジピリジニルおよびアリール−ピリジニル誘導体ならびにその使用 |
| JP2011506462A (ja) * | 2007-12-10 | 2011-03-03 | グラクソ グループ リミテッド | メラニン凝集ホルモン受容体１アンタゴニストとしてのビス−ピリジルピリドン |
| WO2011025799A1 (en) * | 2009-08-26 | 2011-03-03 | Glaxo Group Limited | Cathepsin c inhibitors |
| CA2778484C (en) * | 2009-10-23 | 2018-07-31 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
| MX2012006909A (es) * | 2009-12-29 | 2012-07-10 | Suven Life Sciences Ltd | LIGANDOS DEL RECEPTOR NICOTINICO NEURONAL A4ß2 DE ACETILCOLINA. |
| TW201139406A (en) * | 2010-01-14 | 2011-11-16 | Glaxo Group Ltd | Voltage-gated sodium channel blockers |
| US8486968B2 (en) * | 2010-12-10 | 2013-07-16 | Boehringer Ingelheim International Gmbh | Compounds |
| WO2012123449A1 (en) * | 2011-03-14 | 2012-09-20 | Boehringer Ingelheim International Gmbh | N- cyclopropyl - n- piperidinylbenzamides as gpr119 modulators |
| ES2750640T3 (es) | 2012-08-16 | 2020-03-26 | Scripps Research Inst | Ligandos opioides kappa novedosos |
-
2013
- 2013-08-16 ES ES13829428T patent/ES2750640T3/es active Active
- 2013-08-16 DK DK13829428.5T patent/DK2884978T3/da active
- 2013-08-16 CA CA2882132A patent/CA2882132C/en active Active
- 2013-08-16 EP EP13829428.5A patent/EP2884978B1/en active Active
- 2013-08-16 EP EP19186416.4A patent/EP3584246A1/en not_active Withdrawn
- 2013-08-16 AU AU2013302497A patent/AU2013302497A1/en not_active Abandoned
- 2013-08-16 US US14/421,932 patent/US9682966B2/en active Active
- 2013-08-16 WO PCT/US2013/055313 patent/WO2014028829A1/en not_active Ceased
- 2013-08-16 JP JP2015527656A patent/JP6254163B2/ja active Active
-
2017
- 2017-05-15 US US15/595,436 patent/US10118915B2/en active Active
- 2017-11-29 JP JP2017228495A patent/JP2018058873A/ja active Pending
-
2018
- 2018-03-02 AU AU2018201522A patent/AU2018201522A1/en not_active Abandoned
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2019
- 2019-10-11 AU AU2019246921A patent/AU2019246921B2/en active Active
-
2020
- 2020-01-27 JP JP2020010476A patent/JP2020090518A/ja active Pending
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2024
- 2024-04-04 US US18/627,081 patent/US20250066336A1/en active Pending
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2025
- 2025-07-18 US US19/274,318 patent/US20250346584A1/en active Pending