JP2019519583A5 - - Google Patents
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- JP2019519583A5 JP2019519583A5 JP2018568716A JP2018568716A JP2019519583A5 JP 2019519583 A5 JP2019519583 A5 JP 2019519583A5 JP 2018568716 A JP2018568716 A JP 2018568716A JP 2018568716 A JP2018568716 A JP 2018568716A JP 2019519583 A5 JP2019519583 A5 JP 2019519583A5
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- -1 cyano, hydroxy Chemical group 0.000 claims 27
- 150000001204 N-oxides Chemical class 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 17
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000003226 pyrazolyl 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 206010012335 Dependence Diseases 0.000 claims 2
- 208000012661 Dyskinesia Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 206010002022 amyloidosis Diseases 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 1
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims 1
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- DTCZNKWBDTXEBS-UHFFFAOYSA-N CC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)(F)F)=O)C Chemical compound CC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)(F)F)=O)C DTCZNKWBDTXEBS-UHFFFAOYSA-N 0.000 claims 1
- RJQGPVBHMYZOSM-UHFFFAOYSA-N CC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C=1C=NC=CC=1)=O)C Chemical compound CC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C=1C=NC=CC=1)=O)C RJQGPVBHMYZOSM-UHFFFAOYSA-N 0.000 claims 1
- OTUOXGZVIWSELJ-UHFFFAOYSA-N COCC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)(F)F)=O)C Chemical compound COCC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)(F)F)=O)C OTUOXGZVIWSELJ-UHFFFAOYSA-N 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- KAADPUKOZSAOGP-UHFFFAOYSA-N ClC=1C(=C2C(=NC=1C)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)F)=O)C Chemical compound ClC=1C(=C2C(=NC=1C)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)F)=O)C KAADPUKOZSAOGP-UHFFFAOYSA-N 0.000 claims 1
- YHMUPFLHJYDUGF-UHFFFAOYSA-N ClC=1C(=C2C(=NC=1COC)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)F)=O)C Chemical compound ClC=1C(=C2C(=NC=1COC)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)F)=O)C YHMUPFLHJYDUGF-UHFFFAOYSA-N 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010021639 Incontinence Diseases 0.000 claims 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 1
- YJVGDXXALNHHDY-UHFFFAOYSA-N OCC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)(F)F)=O)C Chemical compound OCC1=CC(=C2C(=N1)CN(C2)C(CC1CN(C1)C1=CC(=NC=C1)C(F)(F)F)=O)C YJVGDXXALNHHDY-UHFFFAOYSA-N 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 102000029797 Prion Human genes 0.000 claims 1
- 108091000054 Prion Proteins 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 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 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims 1
- 125000005057 dihydrothienyl group Chemical group S1C(CC=C1)* 0.000 claims 1
- 125000000532 dioxanyl group Chemical group 0.000 claims 1
- 125000005879 dioxolanyl group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010013781 dry mouth Diseases 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 1
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 1
- 201000008319 inclusion body myositis Diseases 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 208000020658 intracerebral hemorrhage Diseases 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 229960004502 levodopa Drugs 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000000160 oxazolidinyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 210000000578 peripheral nerve Anatomy 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims 1
- 125000001984 thiazolidinyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662357624P | 2016-07-01 | 2016-07-01 | |
| US62/357,624 | 2016-07-01 | ||
| US201662372421P | 2016-08-09 | 2016-08-09 | |
| US62/372,421 | 2016-08-09 | ||
| PCT/IB2017/053565 WO2018002760A1 (en) | 2016-07-01 | 2017-06-15 | 5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019519583A JP2019519583A (ja) | 2019-07-11 |
| JP2019519583A5 true JP2019519583A5 (https=) | 2020-07-27 |
| JP7046018B2 JP7046018B2 (ja) | 2022-04-01 |
Family
ID=59215839
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018568716A Active JP7046018B2 (ja) | 2016-07-01 | 2017-06-15 | 神経性疾患および神経変性疾患を処置するための５，７－ジヒドロピロロピリジン誘導体 |
Country Status (20)
| Country | Link |
|---|---|
| US (5) | US10604519B2 (https=) |
| EP (2) | EP3478679B1 (https=) |
| JP (1) | JP7046018B2 (https=) |
| KR (1) | KR102470497B1 (https=) |
| CN (1) | CN109641898B (https=) |
| AU (1) | AU2017286868B2 (https=) |
| CA (1) | CA2972070C (https=) |
| DK (1) | DK3478679T3 (https=) |
| ES (1) | ES2878160T3 (https=) |
| HU (1) | HUE054857T2 (https=) |
| IL (1) | IL263912B (https=) |
| MX (1) | MX386258B (https=) |
| PH (1) | PH12019500004A1 (https=) |
| PL (1) | PL3478679T3 (https=) |
| PT (1) | PT3478679T (https=) |
| SG (1) | SG11201811712QA (https=) |
| TW (1) | TWI736642B (https=) |
| UY (1) | UY37311A (https=) |
| WO (1) | WO2018002760A1 (https=) |
| ZA (1) | ZA201900519B (https=) |
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| WO2018226545A1 (en) * | 2017-06-09 | 2018-12-13 | Merck Sharp & Dohme Corp. | Azabicyclo[4.1.0]heptane allosteric modulators of the m4 muscarinic acetylcholine receptor |
| IL271290B2 (en) | 2017-06-22 | 2023-11-01 | Pfizer | Dihydro-pyrrolo-pyridine derivatives |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
| EP4061813B1 (en) | 2019-11-22 | 2025-06-04 | F. Hoffmann-La Roche AG | Pyrrolidine derivatives |
| EP4143196A4 (en) * | 2020-04-29 | 2024-04-17 | Relay Therapeutics, Inc. | PI3K-A INHIBITORS AND METHODS OF USE THEREOF |
| CN112174869B (zh) * | 2020-10-12 | 2023-04-25 | 蔡霈 | N-苯乙酰基-2-羟甲基吡咯烷-2-甲酰胺的制备方法及其药用用途 |
| JP2023549738A (ja) * | 2020-10-30 | 2023-11-29 | １シーバイオ， インコーポレイテッド | エクトヌクレオチドピロホスファターゼ－ホスホジエステラーゼ－１（ｅｎｐｐ１）阻害物質及びそれらの使用 |
| WO2022235514A1 (en) * | 2021-05-04 | 2022-11-10 | Mind Medicine, Inc. | Liposome delivery of psychedelics |
| CN120677153A (zh) * | 2022-09-23 | 2025-09-19 | 赛尔维治疗有限责任公司 | Emraclidine的晶型及其制备方法和用途 |
| WO2024088408A1 (zh) * | 2022-10-28 | 2024-05-02 | 纽欧申医药(上海)有限公司 | 一种含氮杂环化合物、其药学上可接受的盐及其制备方法与应用 |
| WO2024130064A1 (en) * | 2022-12-16 | 2024-06-20 | Karuna Therapeutics, Inc. | Substituted tetrahydropyrrolo-pyridinone compounds and their use in treating medical conditions |
| KR20250133677A (ko) * | 2022-12-16 | 2025-09-08 | 카루나 세러퓨틱스 인코포레이티드 | 치환된 디하이드로피롤로[3,4-d]피리미딘 화합물 및 의학적 병태 치료에서의 이의 용도 |
| EP4634181A1 (en) | 2022-12-16 | 2025-10-22 | Karuna Therapeutics, Inc. | Substituted tetrahydropyrrolo-pyridinone compounds and their use in treating medical conditions |
| WO2024130068A1 (en) * | 2022-12-16 | 2024-06-20 | Karuna Therapeutics, Inc. | Substituted dihydropyrrolo [3, 4-d] pyrimidine compounds and their use in treating medical conditions |
| WO2024230794A1 (zh) * | 2023-05-11 | 2024-11-14 | 中国药科大学 | 氮杂环丁烷衍生物、其制备方法及其医药用途 |
| CN116693437A (zh) * | 2023-06-15 | 2023-09-05 | 安徽大学 | 一种N-Boc-3-氮杂环丁烷乙酸的合成方法 |
| AU2024311336A1 (en) * | 2023-06-20 | 2026-01-22 | Haisco Pharmaceutical Group Co., Ltd. | Muscarinic m4 receptor agonist and use thereof |
| WO2025055965A1 (zh) * | 2023-09-13 | 2025-03-20 | 中国药科大学 | 氮杂环丁烷衍生物、其制备方法及其医药用途 |
| WO2025055970A1 (zh) * | 2023-09-15 | 2025-03-20 | 江苏恩华药业股份有限公司 | 氮杂环丁烷衍生物、其制备方法及其医药用途 |
| WO2025083630A1 (en) | 2023-10-19 | 2025-04-24 | Suven Life Sciences Limited | Heteroaromatic compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
| WO2025099660A1 (en) | 2023-11-10 | 2025-05-15 | Suven Life Sciences Limited | Piperidine substituted compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
| TW202540094A (zh) * | 2023-11-17 | 2025-10-16 | 大陸商上海翰森生物醫藥科技有限公司 | 雜環羰基類衍生物調節劑、其製備方法與應用 |
| WO2025122811A1 (en) * | 2023-12-07 | 2025-06-12 | Acadia Pharmaceuticals Inc. | M4 positive allosteric modulators |
| WO2025131049A1 (en) * | 2023-12-21 | 2025-06-26 | Ignis Therapeutics (Suzhou) Limited | Dihydro-pyrrolo-pyridine derivatives and uses thereof |
| WO2025134078A1 (en) | 2023-12-22 | 2025-06-26 | Suven Life Sciences Limited | Organic compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
| TW202525292A (zh) * | 2023-12-27 | 2025-07-01 | 大陸商宜昌人福藥業有限責任公司 | 稠合嘧啶環化合物、藥物組合物及其應用 |
| WO2025145091A1 (en) | 2023-12-29 | 2025-07-03 | Pfizer Inc. | Crystalline forms of a muscarinic m4 receptor modulator and methods of treating diseases |
| WO2025201078A1 (zh) * | 2024-03-25 | 2025-10-02 | 四川科伦药物研究院有限公司 | 化合物、包含其的药物组合物及其制备方法和用途 |
| WO2026012503A1 (zh) * | 2024-07-12 | 2026-01-15 | 海思科医药集团股份有限公司 | 一种毒蕈碱m4受体激动剂及其用途 |
| WO2026017066A1 (zh) * | 2024-07-17 | 2026-01-22 | 中国药科大学 | 取代的氮杂环丁烷衍生物、其制备方法及其医药用途 |
| WO2026017171A1 (zh) * | 2024-07-19 | 2026-01-22 | 上海翰森生物医药科技有限公司 | 杂环羰基类衍生物调节剂、其制备方法和应用 |
| WO2026037961A1 (en) | 2024-08-15 | 2026-02-19 | Neurosterix Pharma Sàrl | 3-cyclopropylpyrazole derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor |
| WO2026037949A1 (en) | 2024-08-15 | 2026-02-19 | Neurosterix Pharma Sàrl | 3-cyclopropylpyrazole derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor |
| WO2026047494A1 (en) | 2024-08-26 | 2026-03-05 | Suven Life Sciences Limited | 2-AMINO-PYRIMIDINE DERIVATIVES AS MUSCARINIC M4 RECEPTOR POSITIVE ALLOSTERIC MODULATORS (M4 PAMs) |
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2017
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- 2017-06-15 EP EP17733044.6A patent/EP3478679B1/en active Active
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- 2017-06-15 JP JP2018568716A patent/JP7046018B2/ja active Active
- 2017-06-15 EP EP21167379.3A patent/EP3872078A1/en active Pending
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