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
Links
- 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) | EP3584246A1 (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 |
|---|---|---|---|---|
| WO2014028829A1 (en) | 2012-08-16 | 2014-02-20 | The Scripps Research Institute | Novel kappa opioid ligands |
| US10982041B2 (en) * | 2016-02-25 | 2021-04-20 | Swancor Advanced Materials Co., Ltd. | Epoxy resin oligomer |
| EA202092442A3 (ru) | 2016-06-07 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| JP7132237B2 (ja) | 2017-03-17 | 2022-09-06 | ザ スクリプス リサーチ インスティテュート | κオピオイド受容体アンタゴニストならびにそれに関連する産物および方法 |
| WO2018172984A1 (en) | 2017-03-23 | 2018-09-27 | Jacobio Pharmaceuticals Co., Ltd. | Novel 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 |
| EP3723751A4 (en) * | 2017-12-08 | 2021-07-07 | The Rockefeller University | KAPPA PYRANO [3,4-B] PYRAZINE OPIOID RECEIVER LIGANDS FOR THE TREATMENT OF ADDICTION, PRURITUS, PAIN AND INFLAMMATION |
| CN112839935A (zh) | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| EP4665455A1 (en) * | 2023-02-17 | 2025-12-24 | The Scripps Research Institute | Quinoline derivatives which act as kappa-opioid receptor antagonists |
| 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 |
| TW202515866A (zh) * | 2023-09-05 | 2025-04-16 | 大陸商西藏海思科製藥有限公司 | Kor拮抗劑及其在醫藥上的應用 |
| 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 |
| US6323212B1 (en) * | 1992-01-23 | 2001-11-27 | Toray Industries, Inc. | Morphinan derivative and its pharmaceutical applications |
| AU1918299A (en) | 1998-02-23 | 1999-09-06 | Warner-Lambert Company | Substituted quinoxaline derivatives as interleukin-8 receptor antagonists |
| BR9909773A (pt) * | 1998-04-20 | 2000-12-19 | Basf Ag | Amida heterociclicamente substituìda, uso da mesma, e, preparação farmacêutica para uso oral, parenteral e intraperitoneal |
| 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 |
| JP4765627B2 (ja) * | 2003-09-22 | 2011-09-07 | Ｍｓｄ株式会社 | 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 |
| ES2354824T3 (es) * | 2004-11-04 | 2011-03-18 | Vertex Pharmaceuticals, Inc. | Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. |
| GB0510204D0 (en) * | 2005-05-19 | 2005-06-22 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| KR101347102B1 (ko) * | 2005-10-19 | 2014-01-03 | 그뤼넨탈 게엠베하 | 신규한 바닐로이드 수용체 리간드 및 약제를 제조하기 위한이의 용도 |
| US8148535B2 (en) * | 2005-10-21 | 2012-04-03 | Merck Sharp & Dohme Corp. | Potassium channel inhibitors |
| CA2669311C (en) | 2006-11-13 | 2011-09-20 | Pfizer Products Inc. | Diaryl, dipyridinyl and aryl-pyridinyl derivatives and uses thereof |
| MX2010006388A (es) * | 2007-12-10 | 2010-06-25 | Glaxo Group Ltd | Bis-piridilpiridonas como antagonistas del receptor 1 de la hormona concentradora de melanina. |
| WO2011025799A1 (en) * | 2009-08-26 | 2011-03-03 | Glaxo Group Limited | Cathepsin c inhibitors |
| ES2585806T3 (es) | 2009-10-23 | 2016-10-10 | Janssen Pharmaceutica N.V. | Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina |
| CA2785957C (en) * | 2009-12-29 | 2015-06-16 | Suven Life Sciences Limited | .alpha.4.beta.2 neuronal nicotinic acetylcholine receptor ligands |
| 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 |
| US8822471B2 (en) * | 2011-03-14 | 2014-09-02 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| WO2014028829A1 (en) | 2012-08-16 | 2014-02-20 | The Scripps Research Institute | Novel kappa opioid ligands |
-
2013
- 2013-08-16 WO PCT/US2013/055313 patent/WO2014028829A1/en not_active Ceased
- 2013-08-16 AU AU2013302497A patent/AU2013302497A1/en not_active Abandoned
- 2013-08-16 DK DK13829428.5T patent/DK2884978T3/da active
- 2013-08-16 JP JP2015527656A patent/JP6254163B2/ja active Active
- 2013-08-16 EP EP19186416.4A patent/EP3584246A1/en not_active Withdrawn
- 2013-08-16 EP EP13829428.5A patent/EP2884978B1/en active Active
- 2013-08-16 ES ES13829428T patent/ES2750640T3/es active Active
- 2013-08-16 CA CA2882132A patent/CA2882132C/en active Active
- 2013-08-16 US US14/421,932 patent/US9682966B2/en 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
-
2019
- 2019-10-11 AU AU2019246921A patent/AU2019246921B2/en active Active
-
2020
- 2020-01-27 JP JP2020010476A patent/JP2020090518A/ja active Pending
-
2024
- 2024-04-04 US US18/627,081 patent/US20250066336A1/en active Pending
-
2025
- 2025-07-18 US US19/274,318 patent/US20250346584A1/en active Pending
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