JP2020532592A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020532592A5 JP2020532592A5 JP2020534818A JP2020534818A JP2020532592A5 JP 2020532592 A5 JP2020532592 A5 JP 2020532592A5 JP 2020534818 A JP2020534818 A JP 2020534818A JP 2020534818 A JP2020534818 A JP 2020534818A JP 2020532592 A5 JP2020532592 A5 JP 2020532592A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- haloalkyl
- halo
- lower alkyl
- alkoxy
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 863
- 125000001188 haloalkyl group Chemical group 0.000 claims description 800
- 125000003545 alkoxy group Chemical group 0.000 claims description 746
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 410
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 264
- 150000001875 compounds Chemical class 0.000 claims description 263
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 190
- 125000001072 heteroaryl group Chemical group 0.000 claims description 118
- 125000003118 aryl group Chemical group 0.000 claims description 108
- 125000000623 heterocyclic group Chemical group 0.000 claims description 72
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 60
- 150000003839 salts Chemical class 0.000 claims description 24
- 239000012453 solvate Substances 0.000 claims description 24
- -1 methoxy, ethoxy, isopropoxy Chemical group 0.000 claims description 17
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 150000004677 hydrates Chemical class 0.000 claims description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 3
- 125000001995 cyclobutyl group Chemical group [H]C1([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
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims 106
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 description 462
- 238000000034 method Methods 0.000 description 30
- 0 *C1*(C(*2CC*(*)CC2)=O)c2cc(N)c(*)c(*)c2C1* Chemical compound *C1*(C(*2CC*(*)CC2)=O)c2cc(N)c(*)c(*)c2C1* 0.000 description 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 14
- 208000035475 disorder Diseases 0.000 description 14
- 208000019901 Anxiety disease Diseases 0.000 description 7
- 230000003557 neuropsychological effect Effects 0.000 description 6
- 230000009286 beneficial effect Effects 0.000 description 4
- 208000020401 Depressive disease Diseases 0.000 description 3
- 230000027288 circadian rhythm Effects 0.000 description 3
- 201000000980 schizophrenia Diseases 0.000 description 3
- 206010013935 Dysmenorrhoea Diseases 0.000 description 2
- 208000019022 Mood disease Diseases 0.000 description 2
- 206010034912 Phobia Diseases 0.000 description 2
- 208000028017 Psychotic disease Diseases 0.000 description 2
- 206010041250 Social phobia Diseases 0.000 description 2
- GXBMIBRIOWHPDT-UHFFFAOYSA-N Vasopressin Natural products N1C(=O)C(CC=2C=C(O)C=CC=2)NC(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C1CC1=CC=CC=C1 GXBMIBRIOWHPDT-UHFFFAOYSA-N 0.000 description 2
- 102000002852 Vasopressins Human genes 0.000 description 2
- 108010004977 Vasopressins Proteins 0.000 description 2
- KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical compound C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 description 2
- 208000024714 major depressive disease Diseases 0.000 description 2
- 208000019899 phobic disease Diseases 0.000 description 2
- 208000028173 post-traumatic stress disease Diseases 0.000 description 2
- 238000001228 spectrum Methods 0.000 description 2
- 230000035882 stress Effects 0.000 description 2
- 229960003726 vasopressin Drugs 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 206010001488 Aggression Diseases 0.000 description 1
- 208000000044 Amnesia Diseases 0.000 description 1
- 208000007415 Anhedonia Diseases 0.000 description 1
- 208000020925 Bipolar disease Diseases 0.000 description 1
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 description 1
- 208000026331 Disruptive, Impulse Control, and Conduct disease Diseases 0.000 description 1
- 208000027534 Emotional disease Diseases 0.000 description 1
- 208000011688 Generalised anxiety disease Diseases 0.000 description 1
- 208000001456 Jet Lag Syndrome Diseases 0.000 description 1
- 208000026139 Memory disease Diseases 0.000 description 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 description 1
- 208000000810 Separation Anxiety Diseases 0.000 description 1
- 201000001880 Sexual dysfunction Diseases 0.000 description 1
- 230000016571 aggressive behavior Effects 0.000 description 1
- 208000012761 aggressive behavior Diseases 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 208000029560 autism spectrum disease Diseases 0.000 description 1
- 230000037326 chronic stress Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 208000024732 dysthymic disease Diseases 0.000 description 1
- 208000029364 generalized anxiety disease Diseases 0.000 description 1
- 150000002431 hydrogen Chemical class 0.000 description 1
- 208000000509 infertility Diseases 0.000 description 1
- 230000036512 infertility Effects 0.000 description 1
- 231100000535 infertility Toxicity 0.000 description 1
- 208000015046 intermittent explosive disease Diseases 0.000 description 1
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 description 1
- 230000006984 memory degeneration Effects 0.000 description 1
- 208000023060 memory loss Diseases 0.000 description 1
- 208000019906 panic disease Diseases 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 208000020016 psychiatric disease Diseases 0.000 description 1
- 208000022610 schizoaffective disease Diseases 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 208000025874 separation anxiety disease Diseases 0.000 description 1
- 231100000872 sexual dysfunction Toxicity 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 208000020685 sleep-wake disease Diseases 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762554452P | 2017-09-05 | 2017-09-05 | |
| US62/554,452 | 2017-09-05 | ||
| PCT/US2018/049607 WO2019050988A1 (en) | 2017-09-05 | 2018-09-05 | ANTAGONISTS OF THE VASOPRESSIN RECEPTOR, PRODUCTS AND RELATED METHODS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020532592A JP2020532592A (ja) | 2020-11-12 |
| JP2020532592A5 true JP2020532592A5 (enExample) | 2021-10-07 |
| JP7368357B2 JP7368357B2 (ja) | 2023-10-24 |
Family
ID=63708454
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020534818A Active JP7368357B2 (ja) | 2017-09-05 | 2018-09-05 | バソプレシン受容体アンタゴニストならびにそれに関連する生成物および方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10538530B2 (enExample) |
| EP (1) | EP3679043B9 (enExample) |
| JP (1) | JP7368357B2 (enExample) |
| KR (1) | KR102765806B1 (enExample) |
| CN (1) | CN111212842B (enExample) |
| AU (1) | AU2018330423B2 (enExample) |
| CA (1) | CA3072766A1 (enExample) |
| ES (1) | ES2951874T3 (enExample) |
| IL (1) | IL272563B2 (enExample) |
| MX (1) | MX2020002436A (enExample) |
| SG (1) | SG11202001498QA (enExample) |
| WO (1) | WO2019050988A1 (enExample) |
| ZA (2) | ZA202001027B (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106810536A (zh) | 2015-11-30 | 2017-06-09 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| PE20231372A1 (es) | 2020-09-03 | 2023-09-07 | Hoffmann La Roche | Compuestos heterociclicos |
| AU2022260537A1 (en) * | 2021-04-23 | 2023-09-21 | F. Hoffmann-La Roche Ag | Heterocyclic compounds |
| IL313987A (en) | 2021-12-29 | 2024-08-01 | Psy Therapeutics Inc | Inhibiting monoacylglycerol lipase (magl) |
| US20250170100A1 (en) * | 2021-12-29 | 2025-05-29 | Psy Therapeutics, Inc. | Monoacylglycerol lipase inhibitors and use thereof for the treatment of anxiety and related conditions |
| WO2023130050A1 (en) * | 2021-12-29 | 2023-07-06 | Psy Therapeutics, Inc. | Monoacylglycerol lipase inhibitors and use thereof for the treatment and management of pain |
| AU2023323878A1 (en) * | 2022-08-11 | 2025-01-30 | Remynd N.V. | (aza)spiroheptane derivatives for the treatment of neurodegenerative disorders |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2025005A (en) * | 1930-01-02 | 1935-12-17 | Union Switch & Signal Co | Multiple control apparatus |
| DE3930262A1 (de) * | 1989-09-11 | 1991-03-21 | Thomae Gmbh Dr K | Kondensierte diazepinone, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| US5091387A (en) * | 1990-03-02 | 1992-02-25 | Merck & Co., Inc. | Spirocyclic oxytocin antagonists |
| JP2003505388A (ja) * | 1999-07-21 | 2003-02-12 | アストラゼネカ・アクチエボラーグ | 新規化合物 |
| CA2581150A1 (en) * | 2004-09-17 | 2006-03-30 | Osi Pharmaceuticals, Inc. | (spirocyclylamido) aminothiophene compounds as c-kit proto- oncogene inhibitors |
| PL1912976T3 (pl) * | 2005-07-21 | 2009-04-30 | Hoffmann La Roche | Pochodne indol-3-ilokarbonylopiperydynobenzoimidazolu jako antagoniści receptora V1a |
| US7351706B2 (en) * | 2006-01-05 | 2008-04-01 | Hoffmann-La Roche Inc. | Indol-3-yl-carbonyl-spiro-piperidine derivatives |
| EP2076517A1 (en) * | 2006-09-22 | 2009-07-08 | Janssen Pharmaceutica N.V. | Spiro benzazepines as vasopressin antagonists |
| JP2010511654A (ja) * | 2006-12-07 | 2010-04-15 | エフ．ホフマン−ラ ロシュ アーゲー | スピロ−ピペリジン誘導体 |
| CN101547923A (zh) * | 2006-12-07 | 2009-09-30 | 弗·哈夫曼-拉罗切有限公司 | 作为via受体拮抗剂的螺环-哌啶衍生物 |
| US8329904B2 (en) | 2009-05-12 | 2012-12-11 | Hoffmann-La Roche Inc. | Azacyclic derivatives |
| KR20120099415A (ko) * | 2009-09-24 | 2012-09-10 | 샤이어-모베티스 엔.브이. | 바소프레신 ｖ２ 리셉터 길항제로서의 (１，４)-벤조디아제핀 |
| US20150376198A1 (en) | 2013-02-18 | 2015-12-31 | The Scripps Research Institute | Modulators of vasopressin receptors with therapeutic potential |
| CN105992587A (zh) | 2013-02-18 | 2016-10-05 | 春堤制药公司 | 作为疫苗佐剂和治疗试剂的短寡核苷酸的设计 |
| US9527856B2 (en) * | 2014-05-15 | 2016-12-27 | AbbVie Deutschland GmbH & Co. KG | Oxindole compounds carrying a CO-bound spiro substituent and use thereof for treating vasopressin-related diseases |
| US9688678B2 (en) * | 2014-05-15 | 2017-06-27 | AbbVie Deutschland GmbH & Co. KG | Oxindole compounds carrying a nitrogen-bound spiro substituent and use thereof for treating vasopressin-related diseases |
| US11186577B2 (en) * | 2017-06-05 | 2021-11-30 | Blackthorn Therapeutics, Inc. | Vasopressin receptor antagonists and products and methods related thereto |
| EP3894414B1 (en) | 2018-12-12 | 2024-04-10 | Neumora Therapeutics, Inc. | 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives as vasopressin antagonists for the treatment of neuro-psychological disorders |
-
2018
- 2018-09-05 SG SG11202001498QA patent/SG11202001498QA/en unknown
- 2018-09-05 KR KR1020207009443A patent/KR102765806B1/ko active Active
- 2018-09-05 CN CN201880057828.7A patent/CN111212842B/zh active Active
- 2018-09-05 WO PCT/US2018/049607 patent/WO2019050988A1/en not_active Ceased
- 2018-09-05 MX MX2020002436A patent/MX2020002436A/es unknown
- 2018-09-05 AU AU2018330423A patent/AU2018330423B2/en active Active
- 2018-09-05 US US16/122,780 patent/US10538530B2/en active Active
- 2018-09-05 CA CA3072766A patent/CA3072766A1/en active Pending
- 2018-09-05 JP JP2020534818A patent/JP7368357B2/ja active Active
- 2018-09-05 ES ES18779495T patent/ES2951874T3/es active Active
- 2018-09-05 EP EP18779495.3A patent/EP3679043B9/en active Active
-
2020
- 2020-02-09 IL IL272563A patent/IL272563B2/en unknown
- 2020-02-18 ZA ZA2020/01027A patent/ZA202001027B/en unknown
-
2021
- 2021-03-05 US US17/194,069 patent/US12152038B2/en active Active
- 2021-06-23 ZA ZA2021/04313A patent/ZA202104313B/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| IL272563B2 (en) | Vasopressin receptor antagonists and related products and methods | |
| JP2022502476A5 (enExample) | ||
| AU2019239955B2 (en) | Kv7 channel activators compositions and methods of use | |
| AU2018274101B2 (en) | Substituted indoline derivatives as dengue viral replication inhibitors | |
| IL291996B1 (en) | Molten bicyclic heteroaromatic compounds active as pesticides | |
| JP2007537251A (ja) | Ｈｉｖインテグラーゼ阻害剤：環状ピリミジノン化合物 | |
| CN106573918A (zh) | 具有抗寄生虫活性的氮杂环庚烷基衍生物和包含它们的药物组合物 | |
| RU2007141632A (ru) | Производные спирооксиндола и их применение в качестве терапевтических агентов | |
| CA2826464A1 (en) | Pharmaceutically active disubstituted triazine derivatives | |
| AU2011235319B2 (en) | Tricyclic compounds and PBK inhibitors containing the same | |
| AR041055A1 (es) | Derivados de benzoimidazol utiles como agentes antiproliferativos, composicion farmaceautica en base al compuesto y un procedimiento de preparacion del compuesto | |
| AU2013224848A1 (en) | Pyrazolo - triazine derivatives as selective cyclin- dependent kinase inhibitors | |
| CA2772989A1 (en) | Sulfonamides as inhibitors of bcl-2 family proteins for the treatment of cancer | |
| JP2021521120A5 (enExample) | ||
| AR063527A1 (es) | Derivados biciclicos fusionados de 2,4-diaminopirimidina como inhibidores de alk y c-met | |
| CZ424798A3 (cs) | Spiropiperidinové deriváty, způsob výroby a farmaceutický prostředek | |
| EP2634189A1 (en) | Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhibitors | |
| WO2024137665A3 (en) | Rubber compositions comprising antidegradants | |
| ES525248A0 (es) | Procedimiento para la produccion de n-fenilsulfonil-n-pirimidinil- y - triacinil-ureas | |
| MX2007012110A (es) | Agentes del receptor de histamina h3, preparacion y usos terapeuticos. | |
| JP2020502089A (ja) | 化合物、組成物および方法 | |
| AU2013302473A1 (en) | Pyrrolopyrazoles as N-type calcium channel blockers | |
| MXPA04007961A (es) | Derivados de pirrolopirimidina. | |
| AU645075B2 (en) | Substituted aromatic sulfonamides as antiglaucoma agents | |
| KR20010071843A (ko) | α2-길항제로서의 트리사이클릭 Δ3-피페리딘 |