CN113056457B - 用于治疗cns疾病的前药 - Google Patents
用于治疗cns疾病的前药 Download PDFInfo
- Publication number
- CN113056457B CN113056457B CN201980075181.5A CN201980075181A CN113056457B CN 113056457 B CN113056457 B CN 113056457B CN 201980075181 A CN201980075181 A CN 201980075181A CN 113056457 B CN113056457 B CN 113056457B
- Authority
- CN
- China
- Prior art keywords
- methyl
- inden
- dihydro
- phenyl
- chloro
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
- C07D295/037—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements with quaternary ring nitrogen 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201800947 | 2018-12-03 | ||
| DKPA201800947 | 2018-12-03 | ||
| PCT/EP2019/082715 WO2020114853A1 (en) | 2018-12-03 | 2019-11-27 | Prodrugs of 4-((1r,3s)-6-chloro-3-phenyl-2,3-dihydro-1h-inden-1-yl)-1,2,2-trimethylpiperazine and 4-((1/r,3s)-6-chloro-3-(phenyl-d5)-2,3-dihydro-1h-inden-1-yl)-2,2-dimethy-1-(methyl-d3)piperazine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN113056457A CN113056457A (zh) | 2021-06-29 |
| CN113056457B true CN113056457B (zh) | 2025-06-20 |
Family
ID=69061245
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980075181.5A Active CN113056457B (zh) | 2018-12-03 | 2019-11-27 | 用于治疗cns疾病的前药 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US11535600B2 (https=) |
| EP (1) | EP3891134A1 (https=) |
| JP (1) | JP7583719B2 (https=) |
| CN (1) | CN113056457B (https=) |
| WO (1) | WO2020114853A1 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020114853A1 (en) | 2018-12-03 | 2020-06-11 | H. Lundbeck A/S | Prodrugs of 4-((1r,3s)-6-chloro-3-phenyl-2,3-dihydro-1h-inden-1-yl)-1,2,2-trimethylpiperazine and 4-((1/r,3s)-6-chloro-3-(phenyl-d5)-2,3-dihydro-1h-inden-1-yl)-2,2-dimethy-1-(methyl-d3)piperazine |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992010192A1 (en) * | 1990-12-04 | 1992-06-25 | H. Lundbeck A/S | Indan derivatives |
| WO2005016901A1 (en) * | 2003-08-18 | 2005-02-24 | H. Lundbeck A/S | Trans-1(6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8427125D0 (en) | 1984-10-26 | 1984-12-05 | Lundbeck & Co As H | Organic compounds |
| ATE60571T1 (de) | 1984-12-04 | 1991-02-15 | Sandoz Ag | Inden-analoga von mevalonolakton und ihre derivate. |
| DK55192D0 (da) * | 1992-04-28 | 1992-04-28 | Lundbeck & Co As H | 1-piperazino-1,2-dihydroindenderivater |
| ES2293638T3 (es) | 1994-03-25 | 2008-03-16 | Isotechnika, Inc. | Mejora de la eficacia de farmacos por deuteracion. |
| US6221335B1 (en) | 1994-03-25 | 2001-04-24 | Isotechnika, Inc. | Method of using deuterated calcium channel blockers |
| WO1999015524A1 (en) | 1997-09-23 | 1999-04-01 | Fujisawa Pharmaceutical Co., Ltd. | Thiazole derivatives |
| US6350786B1 (en) | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
| SE9904850D0 (sv) | 1999-12-30 | 1999-12-30 | Pharmacia & Upjohn Ab | Novel process and intermediates |
| RU2366654C2 (ru) | 2004-06-08 | 2009-09-10 | ЭнЭсЭйБи, ФИЛИАЛ АФ НЕУРОСЕРЧ СВИДЕН АБ, СВЕРИЙЕ | Новые дизамещенные фенилпиперидины/пиперазины в качестве модуляторов допаминовой нейротрансмиссии |
| ES2346452T3 (es) | 2004-06-08 | 2010-10-15 | Nsab, Filial Af Neurosearch Sweden Ab, Sverige | Nuevas fenilpiperidinas/piperazinas disustituidas utilizadas como moduladores de la neurotransmision de la dopamina. |
| WO2006086985A1 (en) | 2005-02-16 | 2006-08-24 | H. Lundbeck A/S | Tartrate and malate salts of trans-1-((1r,3s)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine |
| TWI376373B (en) | 2005-02-16 | 2012-11-11 | Lundbeck & Co As H | Crystalline base of a pharmaceutical compound |
| TWI453198B (zh) | 2005-02-16 | 2014-09-21 | Lundbeck & Co As H | 製造反式-1-((1r,3s)-6-氯基-3-苯基茚滿-1-基) -3 , 3 -二甲基六氫吡與其鹽類之方法及製造4-((1r , 3s)-6 -氯基-3-苯基茚滿-1-基 )-1,2,2-三甲基六氫吡與其鹽類之方法 |
| US7863274B2 (en) | 2005-07-29 | 2011-01-04 | Concert Pharmaceuticals Inc. | Deuterium enriched analogues of tadalafil as PDE5 inhibitors |
| KR101380190B1 (ko) | 2005-07-29 | 2014-04-11 | 콘서트 파마슈티컬즈, 인크. | 벤조 〔d〕〔1,3〕―디옥솔 유도체 |
| PT1954669E (pt) | 2005-12-01 | 2015-10-23 | Auspex Pharmaceuticals Inc | Feniletilaminas substituídas com actividade serotoninérgica e/ou norepinefrinérgica |
| WO2008086158A1 (en) | 2007-01-04 | 2008-07-17 | Smithkline Beecham Corporation | Benzodihydroquinazoline as pi3 kinase inhibitors |
| US8198305B2 (en) | 2007-04-13 | 2012-06-12 | Concert Pharmaceuticals Inc. | 1,2-benzisoxazol-3-yl compounds |
| AU2008242703B2 (en) | 2007-04-19 | 2011-08-18 | Concert Pharmaceuticals Inc. | Deuterated morpholinyl compounds |
| EP1997479A1 (en) | 2007-05-31 | 2008-12-03 | Helm AG | Stabilized amorphous candesartan cilexetil compositions for oral administration |
| US20090062303A1 (en) | 2007-08-29 | 2009-03-05 | Protia, Llc | Deuterium-enriched ziprasidone |
| CN102065861B (zh) | 2008-05-07 | 2013-10-16 | H.隆德贝克有限公司 | 反式-4-((1r,3s)-6-氯-3-苯基茚满-1-基)-1,2,2-三甲基哌嗪用于改善认知的用途 |
| CN102170884A (zh) | 2008-10-03 | 2011-08-31 | H.隆德贝克有限公司 | 口服制剂 |
| JP2012506904A (ja) | 2008-10-28 | 2012-03-22 | エージェンシー フォー サイエンス,テクノロジー アンド リサーチ | 難水溶性成分のためのメソ多孔性材料賦形剤 |
| US20120071554A1 (en) | 2008-10-28 | 2012-03-22 | Liu Julie F | Deuterated 2-propylpentanoic acid compounds |
| TW201102370A (en) * | 2009-07-07 | 2011-01-16 | Lundbeck & Co As H | Manufacture of 4-((1R,3S)-6-chloro-3-phenyl-indan-1-yl)-1,2,2-trimethyl-piperazine and 1-((1R,3S)-6-chloro-3-phenyl-indan-1-yl)-3,3-dimethyl piperazine |
| US8557994B2 (en) | 2009-07-27 | 2013-10-15 | Daljit Singh Dhanoa | Deuterium-enriched pyridinonecarboxamides and derivatives |
| US8658236B2 (en) | 2009-08-21 | 2014-02-25 | Deuteria Beverages, Llc | Alcoholic compositions having a lowered risk of acetaldehydemia |
| KR101149529B1 (ko) | 2009-09-11 | 2012-05-25 | 한국화학연구원 | 인덴온 유도체 및 이를 포함하는 약학적 조성물 |
| CN102020522A (zh) | 2009-09-21 | 2011-04-20 | 陈松源 | 氘代药物的制备方法和应用 |
| WO2011047315A1 (en) | 2009-10-15 | 2011-04-21 | Concert Pharmaceuticals, Inc. | Subsitituted benzimidazoles |
| WO2011059080A1 (ja) | 2009-11-16 | 2011-05-19 | 第一三共株式会社 | 同位体置換されたジアミン誘導体 |
| EP2521711B1 (en) | 2010-01-07 | 2017-08-16 | Alkermes Pharma Ireland Limited | Quaternary ammonium salt prodrugs |
| EP2639216B1 (en) | 2010-11-09 | 2018-07-11 | Kaneka Corporation | Halogenated indenones and method for producing optically active indanones or optically active indanols by using same |
| US20130331575A1 (en) * | 2011-01-07 | 2013-12-12 | Robert Dancer | Method for resolution of 4-((1R,3S)-6-chloro-3-phenyl-indan-1-yl)-1,2,2-trimethyl-piperazine and 1-((1R,3S)-6-chloro-3-phenyl-indan-1-yl)-3,3-dimethyl-piperazine |
| WO2012137225A1 (en) | 2011-04-08 | 2012-10-11 | Sphaera Pharma Pvt. Ltd | Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds |
| DK2720989T3 (en) | 2011-06-20 | 2016-11-28 | H Lundbeck As | Deuterated 1-piperazino-3-phenyl-indanes used to treat schizophrenia |
| AU2013326850B2 (en) | 2012-10-04 | 2017-09-21 | Inhibikase Therapeutics, Inc. | Novel compounds, their preparation and their uses |
| EP2931731A1 (en) * | 2012-12-11 | 2015-10-21 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| AR094054A1 (es) | 2012-12-19 | 2015-07-08 | H Lundbeck As | 6-cloro-3-(fenil-d₅)-inden-1-ona y uso de la misma |
| WO2020089147A1 (en) | 2018-10-29 | 2020-05-07 | H. Lundbeck A/S | Amorphous compounds of formula (i) and amorphous compounds of formula (i) salts |
| WO2020114853A1 (en) | 2018-12-03 | 2020-06-11 | H. Lundbeck A/S | Prodrugs of 4-((1r,3s)-6-chloro-3-phenyl-2,3-dihydro-1h-inden-1-yl)-1,2,2-trimethylpiperazine and 4-((1/r,3s)-6-chloro-3-(phenyl-d5)-2,3-dihydro-1h-inden-1-yl)-2,2-dimethy-1-(methyl-d3)piperazine |
-
2019
- 2019-11-27 WO PCT/EP2019/082715 patent/WO2020114853A1/en not_active Ceased
- 2019-11-27 JP JP2021529329A patent/JP7583719B2/ja active Active
- 2019-11-27 CN CN201980075181.5A patent/CN113056457B/zh active Active
- 2019-11-27 US US17/297,717 patent/US11535600B2/en active Active
- 2019-11-27 EP EP19828958.9A patent/EP3891134A1/en active Pending
-
2022
- 2022-11-23 US US18/058,587 patent/US12071416B2/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992010192A1 (en) * | 1990-12-04 | 1992-06-25 | H. Lundbeck A/S | Indan derivatives |
| WO2005016901A1 (en) * | 2003-08-18 | 2005-02-24 | H. Lundbeck A/S | Trans-1(6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine |
Also Published As
| Publication number | Publication date |
|---|---|
| US20220033367A1 (en) | 2022-02-03 |
| US11535600B2 (en) | 2022-12-27 |
| JP2022509965A (ja) | 2022-01-25 |
| EP3891134A1 (en) | 2021-10-13 |
| US12071416B2 (en) | 2024-08-27 |
| JP7583719B2 (ja) | 2024-11-14 |
| WO2020114853A1 (en) | 2020-06-11 |
| CN113056457A (zh) | 2021-06-29 |
| US20230159478A1 (en) | 2023-05-25 |
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Legal Events
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| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
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| EE01 | Entry into force of recordation of patent licensing contract |
Application publication date: 20210629 Assignee: NHWA PHARMA. Corp. Assignor: H.Lundbeck gmbh Contract record no.: X2022990000498 Denomination of invention: 4-((1R,3S)-6-Chloro-3-phenyl-2,3-dihydro-1H-inden-1-yl)-1,2,2-trimethylpiperazine and 4-(( 1R,3S)-6-Chloro-3-(phenyl-d5)-2,3-dihydro-1H-inden-1-yl)-2,2-dimethyl- Prodrugs of 1-(methyl-d3)piperazine License type: Exclusive License Record date: 20220811 |
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| EE01 | Entry into force of recordation of patent licensing contract | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |