JP6629738B2 - 精神障害の治療のための（ｒ）−３−（（３ｓ，４ｓ）−３−フルオロ−４−（４−ヒドロキシフェニル）ピペリジン−１−イル）−１−（４−メチルベンジル）ピロリジン−２−オンおよびそのプロドラッグ - Google Patents
精神障害の治療のための（ｒ）−３−（（３ｓ，４ｓ）−３−フルオロ−４−（４−ヒドロキシフェニル）ピペリジン−１−イル）−１−（４−メチルベンジル）ピロリジン−２−オンおよびそのプロドラッグ Download PDFInfo
- Publication number
- JP6629738B2 JP6629738B2 JP2016545818A JP2016545818A JP6629738B2 JP 6629738 B2 JP6629738 B2 JP 6629738B2 JP 2016545818 A JP2016545818 A JP 2016545818A JP 2016545818 A JP2016545818 A JP 2016545818A JP 6629738 B2 JP6629738 B2 JP 6629738B2
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- piperidin
- fluoro
- methylbenzyl
- solution
- 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.)
- Expired - Fee Related
Links
- 0 O[C@](C*CC1)[C@@]1c(cc1)ccc1OCc1ccccc1 Chemical compound O[C@](C*CC1)[C@@]1c(cc1)ccc1OCc1ccccc1 0.000 description 3
- BKZYHZZKZXZMCY-QHWQHVLLSA-N C[C@@H](C(Oc1ccc([C@H](CCN(C2)[C@H](CCN3Cc4ccc(C)cc4)C3=O)[C@@H]2F)cc1)=O)NC(OC(C)(C)C)=O Chemical compound C[C@@H](C(Oc1ccc([C@H](CCN(C2)[C@H](CCN3Cc4ccc(C)cc4)C3=O)[C@@H]2F)cc1)=O)NC(OC(C)(C)C)=O BKZYHZZKZXZMCY-QHWQHVLLSA-N 0.000 description 1
- ZPUVTBAQHJFPHE-BHDDXSALSA-N Cc1ccc(CN(CC[C@H]2N(CC[C@H]3c(cc4)ccc4OP(O)(O)=O)C[C@H]3F)C2=O)cc1 Chemical compound Cc1ccc(CN(CC[C@H]2N(CC[C@H]3c(cc4)ccc4OP(O)(O)=O)C[C@H]3F)C2=O)cc1 ZPUVTBAQHJFPHE-BHDDXSALSA-N 0.000 description 1
- CCCWZHVIGUSPFM-OAQYLSRUSA-N OP(O)(Oc1ccc(C(CC2)CCN2[C@H](CCN2Cc(cc3)ccc3F)C2=O)cc1)=O Chemical compound OP(O)(Oc1ccc(C(CC2)CCN2[C@H](CCN2Cc(cc3)ccc3F)C2=O)cc1)=O CCCWZHVIGUSPFM-OAQYLSRUSA-N 0.000 description 1
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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61P25/04—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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/59—Hydrogenated pyridine rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461925405P | 2014-01-09 | 2014-01-09 | |
| US61/925,405 | 2014-01-09 | ||
| PCT/US2015/010552 WO2015105929A1 (en) | 2014-01-09 | 2015-01-08 | (r)-3-((3s,4s)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017503804A JP2017503804A (ja) | 2017-02-02 |
| JP2017503804A5 JP2017503804A5 (enExample) | 2018-02-08 |
| JP6629738B2 true JP6629738B2 (ja) | 2020-01-15 |
Family
ID=52444626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016545818A Expired - Fee Related JP6629738B2 (ja) | 2014-01-09 | 2015-01-08 | 精神障害の治療のための（ｒ）−３−（（３ｓ，４ｓ）−３−フルオロ−４−（４−ヒドロキシフェニル）ピペリジン−１−イル）−１−（４−メチルベンジル）ピロリジン−２−オンおよびそのプロドラッグ |
Country Status (27)
| Country | Link |
|---|---|
| US (10) | US9187506B2 (enExample) |
| EP (2) | EP3677578A1 (enExample) |
| JP (1) | JP6629738B2 (enExample) |
| KR (1) | KR102331120B1 (enExample) |
| AR (1) | AR102019A1 (enExample) |
| AU (1) | AU2015204785A1 (enExample) |
| CA (1) | CA2936338A1 (enExample) |
| CL (1) | CL2016001744A1 (enExample) |
| CY (1) | CY1122768T1 (enExample) |
| DK (1) | DK3092223T3 (enExample) |
| EA (1) | EA201691133A1 (enExample) |
| ES (1) | ES2771825T3 (enExample) |
| HR (1) | HRP20200161T1 (enExample) |
| HU (1) | HUE048750T2 (enExample) |
| IL (1) | IL246596A0 (enExample) |
| LT (1) | LT3092223T (enExample) |
| MX (1) | MX2016008715A (enExample) |
| PE (1) | PE20160898A1 (enExample) |
| PL (1) | PL3092223T3 (enExample) |
| PT (1) | PT3092223T (enExample) |
| RS (1) | RS59858B1 (enExample) |
| SG (1) | SG11201605620QA (enExample) |
| SI (1) | SI3092223T1 (enExample) |
| SM (1) | SMT202000094T1 (enExample) |
| TW (1) | TW201612169A (enExample) |
| UY (1) | UY35946A (enExample) |
| WO (1) | WO2015105929A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9187506B2 (en) * | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
| MX2018004256A (es) | 2015-10-14 | 2018-05-16 | Squibb Bristol Myers Co | Antagonistas de receptor de n-metil-d-aspartato subtipo 2b (nr2b) selectivos. |
| CA3001894A1 (en) * | 2015-10-14 | 2017-04-20 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| US12086719B2 (en) * | 2019-10-11 | 2024-09-10 | Royal Bank Of Canada | System and method of machine learning using embedding networks |
| WO2024197289A1 (en) * | 2023-03-22 | 2024-09-26 | Gilgamesh Pharmaceuticals, Inc. | Negative allosteric modulators of glun2b receptors and methods of making and using the same |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| MXPA02009659A (es) | 2000-04-26 | 2003-03-10 | Warner Lambert Co | Derivado de ciclohexilamina como subtipo de los antagonistas del receptor selectivo nmda. |
| JPWO2003035641A1 (ja) | 2001-10-22 | 2005-02-10 | 塩野義製薬株式会社 | 新規カルバモイルピロリドン誘導体 |
| KR20060017839A (ko) | 2003-06-04 | 2006-02-27 | 머크 앤드 캄파니 인코포레이티드 | Ｎｍｄａ／ｎｒ2ｂ 길항제로서 3-플루오로-피페리딘 |
| MXPA06003748A (es) | 2003-10-08 | 2006-06-14 | Pfizer | Compuestos de lactama condensada. |
| EP2520567A3 (en) | 2006-02-23 | 2012-12-12 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
| KR20100045983A (ko) | 2007-06-29 | 2010-05-04 | 에모리 유니버시티 | 신경보호를 위한 ｎｍｄａ 수용체 길항물질 |
| CN102036985A (zh) * | 2007-11-13 | 2011-04-27 | 沃泰克斯药物股份有限公司 | 用于治疗疼痛的作为离子通道调节剂的4(-3-(-2-(苯基)吗啉代)-2-氧代吡咯烷-1-基)-n-(噻唑-2-基)苯磺酰胺衍生物和相关化合物 |
| US9187506B2 (en) * | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
-
2015
- 2015-01-07 US US14/591,372 patent/US9187506B2/en active Active
- 2015-01-08 SG SG11201605620QA patent/SG11201605620QA/en unknown
- 2015-01-08 TW TW104100590A patent/TW201612169A/zh unknown
- 2015-01-08 CA CA2936338A patent/CA2936338A1/en not_active Abandoned
- 2015-01-08 AU AU2015204785A patent/AU2015204785A1/en not_active Abandoned
- 2015-01-08 MX MX2016008715A patent/MX2016008715A/es unknown
- 2015-01-08 LT LTEP15702312.8T patent/LT3092223T/lt unknown
- 2015-01-08 PE PE2016001105A patent/PE20160898A1/es unknown
- 2015-01-08 DK DK15702312.8T patent/DK3092223T3/da active
- 2015-01-08 JP JP2016545818A patent/JP6629738B2/ja not_active Expired - Fee Related
- 2015-01-08 PL PL15702312T patent/PL3092223T3/pl unknown
- 2015-01-08 SI SI201531064T patent/SI3092223T1/sl unknown
- 2015-01-08 KR KR1020167021355A patent/KR102331120B1/ko not_active Expired - Fee Related
- 2015-01-08 EP EP19212924.5A patent/EP3677578A1/en not_active Withdrawn
- 2015-01-08 HR HRP20200161TT patent/HRP20200161T1/hr unknown
- 2015-01-08 RS RS20200109A patent/RS59858B1/sr unknown
- 2015-01-08 ES ES15702312T patent/ES2771825T3/es active Active
- 2015-01-08 PT PT157023128T patent/PT3092223T/pt unknown
- 2015-01-08 EP EP15702312.8A patent/EP3092223B1/en active Active
- 2015-01-08 WO PCT/US2015/010552 patent/WO2015105929A1/en not_active Ceased
- 2015-01-08 SM SM20200094T patent/SMT202000094T1/it unknown
- 2015-01-08 EA EA201691133A patent/EA201691133A1/ru unknown
- 2015-01-08 HU HUE15702312A patent/HUE048750T2/hu unknown
- 2015-01-09 AR ARP150100067A patent/AR102019A1/es unknown
- 2015-01-09 UY UY0001035946A patent/UY35946A/es unknown
- 2015-10-13 US US14/881,932 patent/US20160030456A1/en not_active Abandoned
-
2016
- 2016-07-04 IL IL246596A patent/IL246596A0/en unknown
- 2016-07-07 CL CL2016001744A patent/CL2016001744A1/es unknown
- 2016-11-21 US US15/357,102 patent/US20170065573A1/en not_active Abandoned
-
2017
- 2017-04-18 US US15/490,558 patent/US20170216325A1/en not_active Abandoned
- 2017-08-17 US US15/679,847 patent/US20170340653A1/en not_active Abandoned
- 2017-12-19 US US15/846,914 patent/US20180104265A1/en not_active Abandoned
-
2018
- 2018-05-04 US US15/971,049 patent/US20180250316A1/en not_active Abandoned
- 2018-12-19 US US16/225,631 patent/US20190125770A1/en not_active Abandoned
-
2019
- 2019-06-27 US US16/454,843 patent/US20190314392A1/en not_active Abandoned
-
2020
- 2020-01-31 US US16/778,960 patent/US20200297742A1/en not_active Abandoned
- 2020-02-07 CY CY20201100120T patent/CY1122768T1/el unknown
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| US9221796B2 (en) | Selective NR2B antagonists | |
| KR101682889B1 (ko) | 치환된 테트라하이드로피란 스피로 피롤리디논 및 피페리디논, 이의 제조방법 및 이의 치료 용도 | |
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