DK3004061T3 - 3,4-dihydroisoquinolin-2(1h)-yl-forbindelser - Google Patents
3,4-dihydroisoquinolin-2(1h)-yl-forbindelser Download PDFInfo
- Publication number
- DK3004061T3 DK3004061T3 DK14732756.3T DK14732756T DK3004061T3 DK 3004061 T3 DK3004061 T3 DK 3004061T3 DK 14732756 T DK14732756 T DK 14732756T DK 3004061 T3 DK3004061 T3 DK 3004061T3
- Authority
- DK
- Denmark
- Prior art keywords
- methyl
- mmol
- compound
- add
- tert
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
- C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
- C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (16)
1. Forbindelse med formlen
hvor n er 0, 1 eller 2; R1 er halogen; R2 er halogen, H, CN, C1 - C3-alkoxy eller C1 - C3-alkyl; og R3 er H, halogen, C1 - C3-alkoxy eller C1 - C3-alkyl.
2. Forbindelse ifølge krav 1 med formlen
hvor n er 0, 1 eller 2; R1 er halogen; R2 er halogen, H, CN, C1 - C3-alkoxy eller C1 - C3-alkyl; og R3 er H, halogen, C1 - C3-alkoxy eller C1 - C3-alkyl.
3. Forbindelse ifølge enten krav 1 eller 2, hvor n er 0, 1 eller 2; R1 er halogen; R2 er halogen; og R3 er hydrogen eller C1 - C3-alkoxy.
4. Forbindelse ifølge enten krav 1 eller 2, hvor n er 0,1 eller 2; R1 er Cl, F eller Br; R2 er Cl, OCH3, H, F, CN eller CH3; og R3 er OCH3, H, CH2CH3, Cl, OCH(CH3)2, OCH2CH3, F, CH(CH3)2 eller CH3.
5. Forbindelse ifølge et af kravene 1,2 eller 3, hvor n er 0 eller 2; R1 er Cl; R2 er Cl eller F; og R3 er H eller OCH3.
6. Forbindelse ifølge krav 1, som er 2-(2,6-dichlorphenyl)-1-[(1S,3R)-3-(hy-droxymethyl)-5-(3-hydroxy-3-methylbutyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl]ethanon.
7. Forbindelse ifølge krav 1, som er 2-(2,6-dichlorphenyl)-1-((1S,3R)-5-(2-hydroxy-2-methylpropyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-on.
8. Sammensætning omfattende 2-(2,6-dichlorphenyl)-1-[(1S,3R)-3-(hydroxy-methyl)-5-(3-hydroxy-3-methylbutyl)-1-methyl-3,4-dihydroisoquinolin-2(1 H)-yl]ethanon og 4-hydroxybenzoesyre.
9. Co-krystallinsk form af sammensætningen ifølge krav 8.
10. Co-krystallinsk form af sammensætningen ifølge krav 9, kendetegnet ved et røntgenpulverdiffraktionsmønster under anvendelse af CuKa-stråling med et diffraktions-peak med diffraktionsvinkel 2-theta på 18,2° i kombination med et eller flere af peaks udvalgt fra gruppen bestående af 16,0°, 25,4° og 7,0°; med en tolerance for diffraktionsvinklerne på 0,2 grader.
11. Co-krystallinsk form af 2-(2,6-dichlorphenyl)-1-((1S,3R)-5-(2-hydroxy-2-methylpropyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1 H)-yl)ethan-1-on og 4-hydroxybenzoesyre.
12. Co-krystallinsk form ifølge krav 11 kendetegnet ved et røntgenpulverdiffraktionsmønster under anvendelse af CuKa-stråling med et diffraktions-peak med diffraktionsvinkel 2-theta på 7,0° i kombination med et eller flere af peaks udvalgt fra gruppen bestående af 18,8°, 16,1 ° og 19,3°; med en tolerance for diffraktionsvinklerne på 0,2 grader.
13. Farmaceutisk sammensætning omfattende en forbindelse ifølge et af kravene 1 til 7, og en farmaceutisk acceptabel bærer, fortyndingsmiddel eller hjælpestof.
14. Forbindelse ifølge et af kravene 1 til 7 til anvendelse inden for behandling.
15. Forbindelse ifølge et af kravene 1 til 7 til anvendelse ved behandling af Parkinsons sygdom.
16. Forbindelse ifølge et af kravene 1 til 7 til anvendelse ved behandling af skizofreni.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361828740P | 2013-05-30 | 2013-05-30 | |
| US201361905329P | 2013-11-18 | 2013-11-18 | |
| PCT/US2014/039494 WO2014193781A1 (en) | 2013-05-30 | 2014-05-27 | 3,4-dihydroisoquinolin-2(1h)-yl compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3004061T3 true DK3004061T3 (da) | 2017-10-23 |
Family
ID=50983199
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK14732756.3T DK3004061T3 (da) | 2013-05-30 | 2014-05-27 | 3,4-dihydroisoquinolin-2(1h)-yl-forbindelser |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US8962654B2 (da) |
| EP (1) | EP3004061B8 (da) |
| JP (2) | JP6130590B2 (da) |
| KR (1) | KR101808933B1 (da) |
| CN (1) | CN105228985B (da) |
| AP (1) | AP2015008867A0 (da) |
| AU (2) | AU2014274435B2 (da) |
| BR (1) | BR112015029090B1 (da) |
| CA (1) | CA2912849C (da) |
| CL (1) | CL2015003444A1 (da) |
| CR (1) | CR20150622A (da) |
| CY (1) | CY1119361T1 (da) |
| DK (1) | DK3004061T3 (da) |
| DO (1) | DOP2015000289A (da) |
| EA (1) | EA029220B1 (da) |
| ES (1) | ES2647086T3 (da) |
| GT (1) | GT201500334A (da) |
| HK (1) | HK1216314A1 (da) |
| HR (1) | HRP20171696T1 (da) |
| HU (1) | HUE034607T2 (da) |
| JO (1) | JO3316B1 (da) |
| LT (1) | LT3004061T (da) |
| ME (1) | ME02838B (da) |
| MX (1) | MX2015016495A (da) |
| MY (1) | MY180751A (da) |
| NZ (1) | NZ713809A (da) |
| PE (1) | PE20152032A1 (da) |
| PH (1) | PH12015502658B1 (da) |
| PL (1) | PL3004061T3 (da) |
| PT (1) | PT3004061T (da) |
| RS (1) | RS56294B1 (da) |
| SG (1) | SG11201509310QA (da) |
| SI (1) | SI3004061T1 (da) |
| TN (1) | TN2015000514A1 (da) |
| TW (2) | TWI691488B (da) |
| UA (1) | UA118759C2 (da) |
| WO (1) | WO2014193781A1 (da) |
| ZA (1) | ZA201508213B (da) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3133070B1 (en) | 2009-11-27 | 2019-08-14 | Genzyme Corporation | Eliglustat (genz 112638) as inhibitor of glucosylceramide synthase for use in a method of treating fabry's or gaucher's disease, the method comprising adjusting the individual therapeutical dose to the p-450 metabolism of the patient |
| JO3316B1 (ar) * | 2013-05-30 | 2019-03-13 | Lilly Co Eli | مركبات 3، 4-داي هيدرو أيزو كوينولين -2(1h)-يل |
| AR106332A1 (es) | 2015-10-23 | 2018-01-03 | Lilly Co Eli | Forma cristalina de 2-(2,6-diclorofenil)-1-[(1s,3r)-3-(hidroximetil)-5-(3-hidroxi-3-metilbutil)-1-metil-3,4-dihidroisoquinolin-2(1h)-il]etanona |
| BR112018070363A2 (pt) | 2016-04-13 | 2019-01-29 | Ucb Biopharma Sprl | derivados de tetraidroisoquinolina |
| EP3585387A4 (en) | 2017-02-21 | 2020-08-12 | Emory University | CHEMIOKIN CXCR4 RECEIVER MODULATORS AND THEIR USES |
| EP3418270A1 (en) | 2017-06-19 | 2018-12-26 | Universidad Complutense De Madrid | Novel biphenylsulfoximines as allosteric modulators of the dopamine d1 receptor |
| EA202091323A1 (ru) * | 2017-12-01 | 2020-10-09 | Юсб Байофарма Срл | Визуализирующие средства |
| TWI725408B (zh) | 2018-04-20 | 2021-04-21 | 美商美國禮來大藥廠 | 多巴胺d1受體正向異位調節劑 |
| US20220062265A1 (en) | 2018-12-18 | 2022-03-03 | Eli Lilly And Company | Dose regimens for use of ly3154207 in the treatment of dopaminergic cns disorders |
| TWI825323B (zh) * | 2019-06-18 | 2023-12-11 | 美商美國禮來大藥廠 | 用於製備2-(2,6-二氯苯基)-1-[(1s,3r)-3-(羥甲基)-5-(3-羥基-3-甲基丁基)-1-甲基-3,4-二氫異喹啉-2(1h)-基]乙烯酮之方法及中間物 |
| US20220259179A1 (en) | 2019-07-01 | 2022-08-18 | UCB Biopharma SRL | A Substituted Tetrahydroisoquinoiline Derivative as a D1 Positive Allosteric Modulator |
| MA56445A (fr) * | 2019-07-01 | 2022-05-11 | UCB Biopharma SRL | Dérivé de tétrahydroisoquinoléine substitué utilisé comme modulateur allostérique positif de d1 |
| MA60976B1 (fr) | 2020-10-07 | 2024-05-31 | Lilly Co Eli | Dérivés de la phényl-3,4-dihydroisoquinoléine-2(1h)-yl-éthan-1-one comme modulateurs allostériques positifs du récepteur d1 de la dopamine |
| EP4267555A1 (en) | 2020-12-03 | 2023-11-01 | UCB Biopharma SRL | Octahydroisoquinolinyl derivatives |
| JP2023553457A (ja) * | 2020-12-18 | 2023-12-21 | ユーシービー バイオファルマ エスアールエル | 非晶質固体分散体 |
| CA3203281A1 (en) * | 2020-12-18 | 2022-06-23 | UCB Biopharma SRL | Prodrugs of 2-(3,5-dichloro-1-methyl-indazol-4-yl)-1-[(1s,3r)-3-(hydroxymethyl)-5-(1-hydroxy-1-methyl-ethyl)-1-methyl-3,4-dihydro-1h-isoquinolin-2-yl]ethanone |
| JP2023554033A (ja) * | 2020-12-18 | 2023-12-26 | ユーシービー バイオファルマ エスアールエル | ジヒドロイソキノリニル誘導体 |
| PE20240632A1 (es) | 2020-12-18 | 2024-03-26 | UCB Biopharma SRL | Un derivado de tetrahidroisoquinolina sustituido como un modulador alosterico positivo de d1 |
| CN117377470A (zh) | 2021-03-08 | 2024-01-09 | 伊莱利利公司 | 美维达林和其他d1正向别构调节剂在幻觉和痴呆相关精神病的治疗中的用途 |
| KR20230154968A (ko) | 2021-03-09 | 2023-11-09 | 일라이 릴리 앤드 캄파니 | 파킨슨병 진행을 늦추기 위한 메비달렌 및 다른 d1 양성 알로스테릭 조절제의 용도 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE68910999T2 (de) | 1988-02-19 | 1994-03-24 | Smithkline Beecham Farma | 1,2,3,4-Tetrahydroisoquinoline, Verfharen zu ihrer Herstellung und ihre Verwendung als Kappa-Rezeptor Agonisten. |
| US5246943A (en) * | 1992-05-19 | 1993-09-21 | Warner-Lambert Company | Substituted 1,2,3,4-tetahydroisoquinolines with angiotensin II receptor antagonist properties |
| US5236934A (en) | 1992-08-26 | 1993-08-17 | E. I. Du Pont De Nemours And Company | 1,2,3,4-tetrahydroisoquinolines useful in the treatment of CNS disorders |
| US5932590A (en) | 1996-12-05 | 1999-08-03 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| ZA991301B (en) | 1998-02-18 | 1999-09-13 | Neurosearch As | Glutamate receptor modulators. |
| CA2408486A1 (en) | 2000-05-11 | 2001-11-15 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs useful as growth hormone secretagogues |
| US7601739B2 (en) | 2003-08-08 | 2009-10-13 | Virgina Commonwealth University | Compounds having antiestrogenic and tissue selective estrogenic properties, and compounds with anti-androgenic properties for treatment of prostate cancer and androgen receptor dependent diseases |
| US7541466B2 (en) | 2003-12-23 | 2009-06-02 | Genzyme Corporation | Tetrahydroisoquinoline derivatives for treating protein trafficking diseases |
| WO2008109336A1 (en) | 2007-03-01 | 2008-09-12 | Janssen Pharmaceutica N.V. | Tetrahydroisoquinoline compounds as modulators of the histamine h3 receptor |
| US20120252853A1 (en) * | 2011-04-01 | 2012-10-04 | H. Lundbeck A/S | Positive allosteric modulators of nicotinic acetylcholine receptor |
| AR089360A1 (es) | 2011-12-21 | 2014-08-20 | Actelion Pharmaceuticals Ltd | Derivados de heterociclilo y su uso como moduladores del receptor d₂ de prostaglandina |
| JO3316B1 (ar) * | 2013-05-30 | 2019-03-13 | Lilly Co Eli | مركبات 3، 4-داي هيدرو أيزو كوينولين -2(1h)-يل |
-
2014
- 2014-05-15 JO JOP/2014/0163A patent/JO3316B1/ar active
- 2014-05-16 TW TW103117402A patent/TWI691488B/zh active
- 2014-05-16 TW TW108104751A patent/TWI691489B/zh active
- 2014-05-27 JP JP2016516713A patent/JP6130590B2/ja active Active
- 2014-05-27 UA UAA201511029A patent/UA118759C2/uk unknown
- 2014-05-27 AU AU2014274435A patent/AU2014274435B2/en active Active
- 2014-05-27 DK DK14732756.3T patent/DK3004061T3/da active
- 2014-05-27 EP EP14732756.3A patent/EP3004061B8/en active Active
- 2014-05-27 BR BR112015029090-6A patent/BR112015029090B1/pt active IP Right Grant
- 2014-05-27 MY MYPI2015704341A patent/MY180751A/en unknown
- 2014-05-27 ES ES14732756.3T patent/ES2647086T3/es active Active
- 2014-05-27 KR KR1020157033616A patent/KR101808933B1/ko active IP Right Grant
- 2014-05-27 SG SG11201509310QA patent/SG11201509310QA/en unknown
- 2014-05-27 NZ NZ71380914A patent/NZ713809A/en unknown
- 2014-05-27 RS RS20170896A patent/RS56294B1/sr unknown
- 2014-05-27 US US14/287,239 patent/US8962654B2/en active Active
- 2014-05-27 CN CN201480031030.7A patent/CN105228985B/zh active Active
- 2014-05-27 PE PE2015002534A patent/PE20152032A1/es unknown
- 2014-05-27 TN TN2015000514A patent/TN2015000514A1/en unknown
- 2014-05-27 MX MX2015016495A patent/MX2015016495A/es active IP Right Grant
- 2014-05-27 AP AP2015008867A patent/AP2015008867A0/xx unknown
- 2014-05-27 EA EA201592082A patent/EA029220B1/ru not_active IP Right Cessation
- 2014-05-27 SI SI201430377T patent/SI3004061T1/sl unknown
- 2014-05-27 PT PT147327563T patent/PT3004061T/pt unknown
- 2014-05-27 CA CA2912849A patent/CA2912849C/en active Active
- 2014-05-27 ME MEP-2017-221A patent/ME02838B/me unknown
- 2014-05-27 LT LTEP14732756.3T patent/LT3004061T/lt unknown
- 2014-05-27 WO PCT/US2014/039494 patent/WO2014193781A1/en active Application Filing
- 2014-05-27 PL PL14732756T patent/PL3004061T3/pl unknown
- 2014-05-27 HU HUE14732756A patent/HUE034607T2/en unknown
-
2015
- 2015-11-06 ZA ZA2015/08213A patent/ZA201508213B/en unknown
- 2015-11-23 CR CR20150622A patent/CR20150622A/es unknown
- 2015-11-24 CL CL2015003444A patent/CL2015003444A1/es unknown
- 2015-11-26 GT GT201500334A patent/GT201500334A/es unknown
- 2015-11-27 DO DO2015000289A patent/DOP2015000289A/es unknown
- 2015-11-27 PH PH12015502658A patent/PH12015502658B1/en unknown
-
2016
- 2016-04-14 HK HK16104287.6A patent/HK1216314A1/zh unknown
- 2016-10-07 AU AU2016238934A patent/AU2016238934B2/en active Active
-
2017
- 2017-04-13 JP JP2017079775A patent/JP6387433B2/ja active Active
- 2017-10-05 CY CY20171101039T patent/CY1119361T1/el unknown
- 2017-11-06 HR HRP20171696TT patent/HRP20171696T1/hr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DK3004061T3 (da) | 3,4-dihydroisoquinolin-2(1h)-yl-forbindelser | |
| CA2999332A1 (en) | Crystalline form of 2-(2,6-dichlorophenyl)-1-[(1s,3r)-3-(hydroxymethyl)-5-(3-hydroxy-3-methylbutyl)-1-methyl-3,4-dihydroisoquinolin-2(1h)-yl]ethanone for the treatment of parkinson's disease | |
| CN102088855A (zh) | 2-芳基甘氨酰胺衍生物 | |
| AU2019256350B2 (en) | Pyrazo-tetrahydroisoquinoline derivatives as dopamine D1 receptor positive modulators | |
| US9981921B2 (en) | Solid forms of substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine compounds | |
| JP5139512B2 (ja) | アミノアルコキシアリールスルホンアミド化合物及び５−ｈｔ６リガンドとしてのその使用 | |
| JP2010515674A (ja) | ５−（ヘテロシクリル）アルキル−ｎ−（アリールスルホニル）インドール化合物および５−ｈｔ６リガンドとしてのそれらの使用 | |
| KR20100047294A (ko) | １-옥소-１,２-디히드로이소퀴놀린-５-카르복스아미드의 유도체 및 ４-옥소-３,４-디히드로퀴나졸린-８-카르복스아미드의 유도체, 그의 제조 및 치료에서의 그의 용도 | |
| CN109651297B (zh) | 一种n-苄基-n-芳基磺酰胺类衍生物及制备和应用 | |
| CN104640853A (zh) | 作为β-淀粉样蛋白抑制剂的吲哚-酰胺化合物 | |
| JP5665537B2 (ja) | ピラゾール３，５カルボキシレート誘導体、これらの調製および治療上の適用 | |
| EA041402B1 (ru) | Производные пиразотетрагидроизохинолина в качестве положительных модуляторов допаминового d1 рецептора |