DK3092224T3 - Selektive nr2b-antagonister - Google Patents
Selektive nr2b-antagonister Download PDFInfo
- Publication number
- DK3092224T3 DK3092224T3 DK15703328.3T DK15703328T DK3092224T3 DK 3092224 T3 DK3092224 T3 DK 3092224T3 DK 15703328 T DK15703328 T DK 15703328T DK 3092224 T3 DK3092224 T3 DK 3092224T3
- Authority
- DK
- Denmark
- Prior art keywords
- piperidin
- pyrrolidin
- fluoro
- hydroxyphenyl
- mmol
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (12)
- SELEKTIVE NR2B-ANTAGONISTER1. Forbindelse med formlen I hvor:Ar1 er phenyl eller indanyl og er substitueret med 0-3 substituenter valgt fra cyano, halo, alkyl, haloalkyl, og haloalkoxy; Ar2 er phenyl substitueret med 1 OH-substituent og ligeledes substitueret med 0-3 substituenter valgt fra cyano, halo, alkyl, haloalkyl og haloalkoxy; X er en binding eller C 1-C3-alkylen; n er 1 eller 2; og ring A er azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, homopiperidinyl eller homopiperazinyl og er substitueret med 0-4 substituenter valgt fra halo, alkyl, hydroxy eller alkoxy; eller et farmaceutisk acceptabelt salt deraf, forudsat at følgende forbindelse er udelukket:
- 2. Forbindelse ifølge krav 1, hvor n er 1 og ring A er piperidinyl substitueret med 0-2 halosubstituenter.
- 3. Forbindelse ifølge krav 1, hvor Ar1 er phenyl substitueret med 0-3 substituenter valgt fra cyano, halo, alkyl, haloalkyl og haloalkoxy.
- 4. Forbindelse ifølge krav 1, hvor Ar2 er p-hydroxyphenyl.
- 5. Forbindelse ifølge krav 1, hvor X er methylen.
- 6. Forbindelse ifølge krav 1, der er valgt fra gruppen bestående af (R)-3-((35',4R)-3-fluor-4-(4-hydroxyphenyl)piperidin-l-yl)-l-(4-methylbenzyl)pyrrolidin-2-on(fo-l-(4-(difluormethyl)benzyl)-3-((3S,45)-3-fluor-4-(4-hydroxyphenyl)piperidin-l-yl)pyrrolidin- 2-onί/ί)- l-id-chloi+enzyll-S-iQS'.dyi-S-niioi'-d-iS-niioiN-hydnixyphenyllpiperidin- l-yl)pyriOlidin-2- on(/?)-l-(4-fluorbenzyl)-3-(4-(4-hydroxyphenyl)piperidin-l-yl)pyrrolidin-2-on3-(3,3-difluor-4-(4-hydroxyphenyl)piperidin-l-yl)-l-(4-methylbenzyl)pyrrolidin-2-oni/i)-3-ii35AS'l-3-niioi'-4-i4-hydi\>xyphenyl)piperidin- 1-yl)- l-i3-niioiN-iiiethylbenzyl)pyn'olidin- 2-on(7?)-3-((37?,47?)-3-fluor-4-(4-hydroxyphenyl)piperidin-l-yl)-l-(3-fluor-4-methylbenzyl)pyrrolidin- 2-on(7?)-3-((37?,47?)-3-fluor-4-(4-hydroxyphenyl)piperidin-l-yl)-l-(4-methylbenzyl)pyrrolidin-2-on(7?)-3-((35,,45,)-3-fluor-4-(3-fluor-4-hydroxyphenyl)piperidin-l-yl)-l-(4-methylbenzyl)pyiTolidin- 2-on(R)-l-(4-(difluormethyl)benzyl)-3-((35',45')-3-fluor-4-(3-fluor-4-hydroxyphenyl)piperidin-l- yl)pyrrolidin-2-onog (R)-l-(4-fluorbenzyl)-3-((35',45')-3-hydroxy-4-(4-methoxyphenyl)piperidin-l-yl)pyrrolidin-2-oneller et farmaceutisk acceptabelt salt deraf.
- 7. Forbindelse ifølge krav 1: (R)-3-((3S,4S)-3-fluor-4-(4-hydroxyphenyl)piperidin-l-yl)-l-(4-methylbenzyl)pyrrolidin-2-on eller et farmaceutisk acceptabelt salt deraf
- 8. Farmaceutisk sammensætning, der omfatter en forbindelse ifølge et hvilket som helst af kravene 1 til 7 eller et farmaceutisk acceptabelt salt deraf og en farmaceutisk acceptabel bærer.
- 9. Forbindelse ifølge et hvilket som helst af kravene 1 til 7 eller et farmaceutisk acceptabelt salt deraf til anvendelse i en fremgangsmåde til behandling af depression, Alzheimers sygdom, neuropatisk smerte eller Parkinsons sygdom.
- 10. Forbindelse til anvendelse ifølge krav 9 rettet mod behandling af depression.
- 11. Forbindelse til anvendelse ifølge krav 9 rettet mod behandling af Alzheimers sygdom.
- 12. Forbindelse til anvendelse ifølge krav 9 rettet mod behandling af neuropatisk smerte.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461925363P | 2014-01-09 | 2014-01-09 | |
| PCT/US2015/010262 WO2015105772A1 (en) | 2014-01-09 | 2015-01-06 | Selective nr2b antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3092224T3 true DK3092224T3 (da) | 2018-11-26 |
Family
ID=52463126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK15703328.3T DK3092224T3 (da) | 2014-01-09 | 2015-01-06 | Selektive nr2b-antagonister |
Country Status (27)
| Country | Link |
|---|---|
| US (10) | US9221796B2 (da) |
| EP (1) | EP3092224B1 (da) |
| JP (1) | JP6543259B2 (da) |
| KR (1) | KR102311518B1 (da) |
| CN (1) | CN106061961B (da) |
| AR (1) | AR099071A1 (da) |
| AU (1) | AU2015205001A1 (da) |
| CA (1) | CA2936293A1 (da) |
| CL (1) | CL2016001763A1 (da) |
| DK (1) | DK3092224T3 (da) |
| EA (1) | EA201691413A1 (da) |
| ES (1) | ES2693250T3 (da) |
| HR (1) | HRP20181585T1 (da) |
| HU (1) | HUE041986T2 (da) |
| IL (1) | IL246599A0 (da) |
| LT (1) | LT3092224T (da) |
| MX (1) | MX2016008898A (da) |
| PE (1) | PE20160933A1 (da) |
| PL (1) | PL3092224T3 (da) |
| PT (1) | PT3092224T (da) |
| RS (1) | RS57830B1 (da) |
| SG (1) | SG11201605618WA (da) |
| SI (1) | SI3092224T1 (da) |
| TR (1) | TR201815579T4 (da) |
| TW (1) | TWI640515B (da) |
| UY (1) | UY35947A (da) |
| WO (1) | WO2015105772A1 (da) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9221796B2 (en) * | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
| AU2016340239A1 (en) * | 2015-10-14 | 2018-05-31 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
| EP3362441B1 (en) | 2015-10-14 | 2020-08-12 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| CN108203404A (zh) * | 2018-03-02 | 2018-06-26 | 上海博邦医药科技有限公司 | (r)-3-苯基哌啶或/和(s)-3-苯基哌啶以及尼拉帕尼的手性中间体的合成方法 |
| US10781172B2 (en) | 2018-06-21 | 2020-09-22 | Northwestern University | Catalysts and methods for enantioselective conjugate additions of amines to unsaturated electrophiles |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2744448B1 (fr) | 1996-02-02 | 1998-04-24 | Pf Medicament | Nouvelles piperidines derivees d'aryl piperazine, ainsi que leur procede de preparation, les compositions pharmaceutiques et leur utilisation comme medicaments |
| AU3818900A (en) | 1999-04-14 | 2000-11-02 | F. Hoffmann-La Roche Ag | Process for the preparation of substituted piperidines |
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| KR20020093950A (ko) * | 2000-04-26 | 2002-12-16 | 워너-램버트 캄파니 | 아형 선택적인 ｎｍｄａ 수용체 길항제로서의시클로헥실아민 유도체 |
| WO2003035641A1 (fr) | 2001-10-22 | 2003-05-01 | Shionogi & Co., Ltd. | Nouveau derive carbamoyl-pyrrolidone |
| CA2527093C (en) | 2003-06-04 | 2009-10-20 | Merck & Co., Inc. | 3-fluoro-piperidines as nmda/nr2b antagonists |
| WO2005035523A1 (en) | 2003-10-08 | 2005-04-21 | Pfizer Japan Inc. | Fused lactam compounds |
| EP1988077A4 (en) | 2006-02-23 | 2009-09-02 | Shionogi & Co | NUCLEIC HETEROCYCLIC DERIVATIVES SUBSTITUTED BY CYCLIC GROUPS |
| CN101815518B (zh) | 2007-06-29 | 2013-01-09 | 埃莫里大学 | 用于神经保护的nmda受体拮抗剂 |
| US9221796B2 (en) * | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
-
2015
- 2015-01-05 US US14/589,205 patent/US9221796B2/en active Active
- 2015-01-06 HU HUE15703328A patent/HUE041986T2/hu unknown
- 2015-01-06 MX MX2016008898A patent/MX2016008898A/es unknown
- 2015-01-06 DK DK15703328.3T patent/DK3092224T3/da active
- 2015-01-06 SG SG11201605618WA patent/SG11201605618WA/en unknown
- 2015-01-06 LT LTEP15703328.3T patent/LT3092224T/lt unknown
- 2015-01-06 EA EA201691413A patent/EA201691413A1/ru unknown
- 2015-01-06 CN CN201580012735.9A patent/CN106061961B/zh active Active
- 2015-01-06 CA CA2936293A patent/CA2936293A1/en not_active Abandoned
- 2015-01-06 AU AU2015205001A patent/AU2015205001A1/en not_active Abandoned
- 2015-01-06 EP EP15703328.3A patent/EP3092224B1/en active Active
- 2015-01-06 WO PCT/US2015/010262 patent/WO2015105772A1/en active Application Filing
- 2015-01-06 JP JP2016545819A patent/JP6543259B2/ja not_active Expired - Fee Related
- 2015-01-06 PE PE2016001107A patent/PE20160933A1/es not_active Application Discontinuation
- 2015-01-06 KR KR1020167021356A patent/KR102311518B1/ko active IP Right Grant
- 2015-01-06 PT PT15703328T patent/PT3092224T/pt unknown
- 2015-01-06 TR TR2018/15579T patent/TR201815579T4/tr unknown
- 2015-01-06 RS RS20181296A patent/RS57830B1/sr unknown
- 2015-01-06 ES ES15703328.3T patent/ES2693250T3/es active Active
- 2015-01-06 SI SI201530408T patent/SI3092224T1/sl unknown
- 2015-01-06 PL PL15703328T patent/PL3092224T3/pl unknown
- 2015-01-08 TW TW104100592A patent/TWI640515B/zh not_active IP Right Cessation
- 2015-01-09 AR ARP150100065A patent/AR099071A1/es unknown
- 2015-01-09 UY UY0001035947A patent/UY35947A/es unknown
- 2015-10-13 US US14/882,041 patent/US20160081995A1/en not_active Abandoned
-
2016
- 2016-07-04 IL IL246599A patent/IL246599A0/en unknown
- 2016-07-08 CL CL2016001763A patent/CL2016001763A1/es unknown
-
2017
- 2017-05-25 US US15/604,904 patent/US20170258777A1/en not_active Abandoned
- 2017-09-15 US US15/706,172 patent/US20180000807A1/en not_active Abandoned
- 2017-12-19 US US15/846,672 patent/US20180110766A1/en not_active Abandoned
-
2018
- 2018-05-04 US US15/971,067 patent/US20180250283A1/en not_active Abandoned
- 2018-10-03 HR HRP20181585TT patent/HRP20181585T1/hr unknown
- 2018-12-19 US US16/225,850 patent/US20190117638A1/en not_active Abandoned
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2019
- 2019-06-27 US US16/454,831 patent/US20190314358A1/en not_active Abandoned
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2020
- 2020-01-30 US US16/777,114 patent/US20200163949A1/en not_active Abandoned
- 2020-09-04 US US17/012,781 patent/US20210121453A1/en not_active Abandoned
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