JPWO2020247445A5 - - Google Patents
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- JPWO2020247445A5 JPWO2020247445A5 JP2021569903A JP2021569903A JPWO2020247445A5 JP WO2020247445 A5 JPWO2020247445 A5 JP WO2020247445A5 JP 2021569903 A JP2021569903 A JP 2021569903A JP 2021569903 A JP2021569903 A JP 2021569903A JP WO2020247445 A5 JPWO2020247445 A5 JP WO2020247445A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- halogen
- substituted
- optionally
- 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 description 156
- 229910052736 halogen Inorganic materials 0.000 claims description 132
- 150000002367 halogens Chemical class 0.000 claims description 132
- 125000003118 aryl group Chemical group 0.000 claims description 124
- 125000001424 substituent group Chemical group 0.000 claims description 108
- 150000001875 compounds Chemical class 0.000 claims description 79
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 62
- 229910052731 fluorine Inorganic materials 0.000 claims description 60
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims description 50
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 48
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 48
- 229910052794 bromium Inorganic materials 0.000 claims description 48
- 229910052801 chlorine Inorganic materials 0.000 claims description 48
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 48
- 229910052740 iodine Inorganic materials 0.000 claims description 48
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 48
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 47
- 150000003839 salts Chemical class 0.000 claims description 41
- 125000001072 heteroaryl group Chemical group 0.000 claims description 39
- 239000012453 solvate Substances 0.000 claims description 38
- 229910052799 carbon Inorganic materials 0.000 claims description 36
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 24
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 24
- 125000004432 carbon atom Chemical group C* 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 24
- 125000003107 substituted aryl group Chemical group 0.000 claims description 24
- 125000001153 fluoro group Chemical group F* 0.000 claims description 22
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 14
- 125000004122 cyclic group Chemical group 0.000 claims description 12
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 12
- 125000002971 oxazolyl group Chemical group 0.000 claims description 12
- 125000003386 piperidinyl group Chemical group 0.000 claims description 12
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 12
- 125000004076 pyridyl group Chemical group 0.000 claims description 12
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 12
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 12
- 125000000335 thiazolyl group Chemical group 0.000 claims description 12
- 125000001544 thienyl group Chemical group 0.000 claims description 12
- 125000001425 triazolyl group Chemical group 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 6
- 210000003169 central nervous system Anatomy 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 6
- 101100097467 Arabidopsis thaliana SYD gene Proteins 0.000 claims description 4
- 101100495925 Schizosaccharomyces pombe (strain 972 / ATCC 24843) chr3 gene Proteins 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 3
- 206010003805 Autism Diseases 0.000 claims description 3
- 208000020706 Autistic disease Diseases 0.000 claims description 3
- 230000036506 anxiety Effects 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 208000035475 disorder Diseases 0.000 claims description 3
- 206010013663 drug dependence Diseases 0.000 claims description 3
- 150000004677 hydrates Chemical class 0.000 claims description 3
- 230000004770 neurodegeneration Effects 0.000 claims description 3
- 201000000980 schizophrenia Diseases 0.000 claims description 3
- 208000011117 substance-related disease Diseases 0.000 claims description 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- -1 carrier Substances 0.000 claims description 2
- QWXYZCJEXYQNEI-OSZHWHEXSA-N intermediate I Chemical compound COC(=O)[C@@]1(C=O)[C@H]2CC=[N+](C\C2=C\C)CCc2c1[nH]c1ccccc21 QWXYZCJEXYQNEI-OSZHWHEXSA-N 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- MEKOFIRRDATTAG-UHFFFAOYSA-N 2,2,5,8-tetramethyl-3,4-dihydrochromen-6-ol Chemical compound C1CC(C)(C)OC2=C1C(C)=C(O)C=C2C MEKOFIRRDATTAG-UHFFFAOYSA-N 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962856830P | 2019-06-04 | 2019-06-04 | |
| US62/856,830 | 2019-06-04 | ||
| PCT/US2020/035848 WO2020247445A1 (en) | 2019-06-04 | 2020-06-03 | Imidazolo derivatives, compositions and methods as orexin antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022534704A JP2022534704A (ja) | 2022-08-03 |
| JP2022534704A5 JP2022534704A5 (https=) | 2023-06-08 |
| JPWO2020247445A5 true JPWO2020247445A5 (https=) | 2023-06-08 |
Family
ID=73652477
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021569903A Pending JP2022534704A (ja) | 2019-06-04 | 2020-06-03 | オレキシンアンタゴニストとしてのイミダゾロ誘導体、組成物、及び方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US12187737B2 (https=) |
| EP (1) | EP3972588A4 (https=) |
| JP (1) | JP2022534704A (https=) |
| KR (1) | KR20220016918A (https=) |
| CN (1) | CN114286675A (https=) |
| AU (1) | AU2020286381C1 (https=) |
| CA (1) | CA3140170A1 (https=) |
| SG (1) | SG11202112827QA (https=) |
| WO (1) | WO2020247445A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114286675A (zh) | 2019-06-04 | 2022-04-05 | 海格生物科学有限责任公司 | 作为食欲肽拮抗剂的咪唑衍生物、组合物以及方法 |
| US20220315602A1 (en) * | 2019-06-04 | 2022-10-06 | Hager Biosciences, Llc | Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists |
| AU2020407664A1 (en) | 2019-12-20 | 2022-08-18 | Tenaya Therapeutics, Inc. | Fluoroalkyl-oxadiazoles and uses thereof |
| AU2022270657A1 (en) | 2021-05-04 | 2023-11-16 | Tenaya Therapeutics, Inc. | 2-fluoroalkyl-1,3,4-oxadiazol-5-yl-thiazol, hdac6 inhibitors for use in the treatment of metabolic disease and hfpef |
| GB202311280D0 (en) | 2023-07-21 | 2023-09-06 | Bial Portela & Ca Sa | Orexin receptor antagonists |
| GB202311281D0 (en) | 2023-07-21 | 2023-09-06 | Bial Portela & Ca Sa | Orexin receptor antagonists |
| WO2025101004A1 (ko) * | 2023-11-08 | 2025-05-15 | 한양대학교 에리카산학협력단 | 6-aryl imidazo[2,1-b]thi/oxazole-2-carboxilic acid 유도체 및 이를 유효성분으로 함유하는 알츠하이머병 치료용 약학 조성물 |
| WO2025188753A1 (en) * | 2024-03-05 | 2025-09-12 | Hager Biosciences, Llc | Pyrazole and imidazole derivatives as dual orexin and kappa-opioid receptors modulators, compositions, and methods for treating neurological and psychiatric disorders |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH02237988A (ja) | 1988-11-18 | 1990-09-20 | Nissan Chem Ind Ltd | イソオキサゾロピリジン系メバロノラクトン類 |
| US5750542A (en) | 1993-09-28 | 1998-05-12 | Pfizer | Benzisoxazole and benzisothizole derivatives as cholinesterase inhibitors |
| JP3810097B2 (ja) | 1993-01-15 | 2006-08-16 | 明治製菓株式会社 | ピロリジン−２−イルカルボニル複素環式化合物誘導体 |
| ES2196806T3 (es) | 1998-05-08 | 2003-12-16 | Smithkline Beecham Plc | Derivados de fenilurea y de feniltiourea. |
| TR200101754T2 (tr) | 1998-12-18 | 2002-05-21 | Schering Corporation | Farnezil protein transferaz inhibitörleri |
| GB0004297D0 (en) | 2000-02-23 | 2000-04-12 | Ucb Sa | 2-oxo-1 pyrrolidine derivatives process for preparing them and their uses |
| US6677354B2 (en) | 2000-06-16 | 2004-01-13 | Smithkline Beecham P.L.C. | Piperdines for use as orexin receptor antagonists |
| JP4246490B2 (ja) | 2000-11-28 | 2009-04-02 | スミスクライン ビーチャム ピー エル シー | オレキシン受容体のアンタゴニストとしてのモルホリン誘導体 |
| IL158463A0 (en) | 2001-05-05 | 2004-05-12 | Smithkline Beecham Plc | N-aroyl cyclic amines |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| GB0130393D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| US7057042B2 (en) | 2002-05-29 | 2006-06-06 | Abbott Laboratories | Fused bicyclic aromatic compounds that are useful in treating sexual dysfunction |
| US20060040937A1 (en) | 2002-09-18 | 2006-02-23 | Glaxo Group Limited | N-aroyl cyclic amines as orexin receptor antagonists |
| US20080119515A1 (en) * | 2003-03-10 | 2008-05-22 | M Arshad Siddiqui | Heterocyclic Kinase Inhibitors: Methods of Use and Synthesis |
| UA85937C2 (uk) | 2004-12-21 | 2009-03-10 | Пфайзер Продактс Інк. | Макроліди |
| DE102005016547A1 (de) | 2005-04-08 | 2006-10-12 | Grünenthal GmbH | Substituierte 5,6,7,8-Tetrahydro-imidazo(1,2-a)pyridin-2-ylamin-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| WO2006127550A1 (en) | 2005-05-23 | 2006-11-30 | Merck & Co., Inc. | Proline bis-amide orexin receptor antagonists |
| UA106873C2 (uk) * | 2006-12-01 | 2014-10-27 | Мерк Шарп Енд Доме Корп. | Сполуки заміщених діазепанів як антагоністи орексинових рецепторів |
| PE20081229A1 (es) | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| JP4881476B2 (ja) | 2007-05-23 | 2012-02-22 | メルク・シャープ・エンド・ドーム・コーポレイション | ピリジルピペリジン・オレキシン受容体アンタゴニスト |
| ATE524466T1 (de) | 2007-07-03 | 2011-09-15 | Actelion Pharmaceuticals Ltd | 3-azabicycloä3.3.0üoktanverbindungen |
| CA2695742C (en) | 2007-08-10 | 2012-11-27 | Rudolf Mueller | Bicyclic amides for enhancing glutamatergic synaptic responses |
| FR2925907B1 (fr) | 2008-01-02 | 2010-10-15 | Sanofi Aventis | DERIVES DE 2-HETEROAROYL-IMIDAZO°1,2-a!PYRIDINE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| EP2252587B1 (en) | 2008-02-12 | 2011-07-20 | F. Hoffmann-La Roche AG | Piperidine sulfonamide derivatives |
| EP2350061B1 (en) | 2008-10-21 | 2013-08-14 | Merck Sharp & Dohme Corp. | 2,3-disubstituted piperidine orexin receptor antagonists |
| AU2009307913A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| EP2349269A4 (en) | 2008-10-21 | 2012-04-25 | Merck Sharp & Dohme | 2,5-DISUBSTITUTED PIPERIDINOREXINE RECEPTOR ANTAGONISTS |
| WO2010141275A1 (en) | 2009-06-01 | 2010-12-09 | Merck Sharp & Dohme Corp. | Pyrazine carboxamide orexin receptor antagonists |
| US20120101106A1 (en) | 2009-07-09 | 2012-04-26 | Mercer Swati P | Tetrahydronapthyridine Orexin Receptor Antagonists |
| WO2011100614A1 (en) | 2010-02-11 | 2011-08-18 | Vanderbilt University | BENZISOXAZOLES AND AZABENZISOXAZOLES AS mgluR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION |
| UA109457C2 (ru) * | 2010-10-21 | 2015-08-25 | Байєр Інтелекчуал Проперті Гмбх | 1-(гетероциклический карбонил)-2-замещенные пирролидины |
| US20120165339A1 (en) | 2010-12-22 | 2012-06-28 | Eisai R&D Management Co., Ltd. | Cyclopropane derivatives |
| KR101873083B1 (ko) * | 2011-02-18 | 2018-06-29 | 이도르시아 파마슈티컬스 리미티드 | 오렉신 길항제로서 유용한 신규 피라졸 및 이미다졸 유도체 |
| EP2730573A4 (en) | 2011-07-05 | 2014-12-03 | Taisho Pharmaceutical Co Ltd | METHYLPIPERIDINDERIVAT |
| WO2013062858A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Isoxazolopyridine orexin receptor antagonists |
| ES2672732T3 (es) | 2012-02-07 | 2018-06-15 | Eolas Therapeutics Inc. | Prolinas/piperidinas sustituidas como antagonistas del receptor de orexina |
| TW201444849A (zh) * | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| EP3083569B1 (en) | 2013-12-20 | 2022-01-26 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| US10081624B2 (en) * | 2014-08-26 | 2018-09-25 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| CN114286675A (zh) | 2019-06-04 | 2022-04-05 | 海格生物科学有限责任公司 | 作为食欲肽拮抗剂的咪唑衍生物、组合物以及方法 |
| US20220315602A1 (en) | 2019-06-04 | 2022-10-06 | Hager Biosciences, Llc | Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists |
-
2020
- 2020-06-03 CN CN202080055282.9A patent/CN114286675A/zh active Pending
- 2020-06-03 EP EP20818543.9A patent/EP3972588A4/en not_active Withdrawn
- 2020-06-03 US US17/616,152 patent/US12187737B2/en active Active
- 2020-06-03 CA CA3140170A patent/CA3140170A1/en active Pending
- 2020-06-03 SG SG11202112827QA patent/SG11202112827QA/en unknown
- 2020-06-03 KR KR1020217043400A patent/KR20220016918A/ko not_active Ceased
- 2020-06-03 WO PCT/US2020/035848 patent/WO2020247445A1/en not_active Ceased
- 2020-06-03 JP JP2021569903A patent/JP2022534704A/ja active Pending
- 2020-06-03 AU AU2020286381A patent/AU2020286381C1/en not_active Expired - Fee Related
-
2024
- 2024-08-12 US US18/800,565 patent/US12187738B2/en active Active
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