JP2017502063A5 - - Google Patents
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- Publication number
- JP2017502063A5 JP2017502063A5 JP2016545819A JP2016545819A JP2017502063A5 JP 2017502063 A5 JP2017502063 A5 JP 2017502063A5 JP 2016545819 A JP2016545819 A JP 2016545819A JP 2016545819 A JP2016545819 A JP 2016545819A JP 2017502063 A5 JP2017502063 A5 JP 2017502063A5
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- piperidin
- hydroxyphenyl
- pyrrolidin
- compound
- 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
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- -1 homopiperidinyl Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- PHZMUXNFZNBYCK-BHDDXSALSA-N (3R)-1-[(4-fluorophenyl)methyl]-3-[(3S,4S)-3-hydroxy-4-(4-methoxyphenyl)piperidin-1-yl]pyrrolidin-2-one Chemical compound FC1=CC=C(CN2C([C@@H](CC2)N2C[C@H]([C@@H](CC2)C2=CC=C(C=C2)OC)O)=O)C=C1 PHZMUXNFZNBYCK-BHDDXSALSA-N 0.000 claims 1
- QGVLIVYFBAIXBS-DFQSSKMNSA-N (3R)-1-[[4-(difluoromethyl)phenyl]methyl]-3-[(3S,4S)-3-fluoro-4-(3-fluoro-4-hydroxyphenyl)piperidin-1-yl]pyrrolidin-2-one Chemical compound FC(C1=CC=C(CN2C([C@@H](CC2)N2C[C@H]([C@@H](CC2)C2=CC(=C(C=C2)O)F)F)=O)C=C1)F QGVLIVYFBAIXBS-DFQSSKMNSA-N 0.000 claims 1
- GCQLNUHXJBJHGL-PWRODBHTSA-N (3R)-1-[[4-(difluoromethyl)phenyl]methyl]-3-[(3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl]pyrrolidin-2-one Chemical compound FC(C1=CC=C(CN2C([C@@H](CC2)N2C[C@H]([C@@H](CC2)C2=CC=C(C=C2)O)F)=O)C=C1)F GCQLNUHXJBJHGL-PWRODBHTSA-N 0.000 claims 1
- LAKBGWVRKNIOGO-BAGYTPMASA-N (3R)-3-[(3R,4R)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl]-1-[(3-fluoro-4-methylphenyl)methyl]pyrrolidin-2-one Chemical compound F[C@H]1CN(CC[C@@H]1C1=CC=C(C=C1)O)[C@H]1C(N(CC1)CC1=CC(=C(C=C1)C)F)=O LAKBGWVRKNIOGO-BAGYTPMASA-N 0.000 claims 1
- UNVYDSCXINFREZ-BHIFYINESA-N (3R)-3-[(3R,4R)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl]-1-[(4-methylphenyl)methyl]pyrrolidin-2-one Chemical compound F[C@H]1CN(CC[C@@H]1C1=CC=C(C=C1)O)[C@H]1C(N(CC1)CC1=CC=C(C=C1)C)=O UNVYDSCXINFREZ-BHIFYINESA-N 0.000 claims 1
- UNVYDSCXINFREZ-YPAWHYETSA-N (3R)-3-[(3S,4R)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl]-1-[(4-methylphenyl)methyl]pyrrolidin-2-one Chemical compound F[C@@H]1CN(CC[C@@H]1C1=CC=C(C=C1)O)[C@H]1C(N(CC1)CC1=CC=C(C=C1)C)=O UNVYDSCXINFREZ-YPAWHYETSA-N 0.000 claims 1
- UMMNFALVRYANIF-CEWLAPEOSA-N (3R)-3-[(3S,4S)-3-fluoro-4-(3-fluoro-4-hydroxyphenyl)piperidin-1-yl]-1-[(4-methylphenyl)methyl]pyrrolidin-2-one Chemical compound F[C@@H]1CN(CC[C@H]1C1=CC(=C(C=C1)O)F)[C@H]1C(N(CC1)CC1=CC=C(C=C1)C)=O UMMNFALVRYANIF-CEWLAPEOSA-N 0.000 claims 1
- LAKBGWVRKNIOGO-KSEOMHKRSA-N (3R)-3-[(3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl]-1-[(3-fluoro-4-methylphenyl)methyl]pyrrolidin-2-one Chemical compound F[C@@H]1CN(CC[C@H]1C1=CC=C(C=C1)O)[C@H]1C(N(CC1)CC1=CC(=C(C=C1)C)F)=O LAKBGWVRKNIOGO-KSEOMHKRSA-N 0.000 claims 1
- UNVYDSCXINFREZ-BHDDXSALSA-N (3R)-3-[(3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl]-1-[(4-methylphenyl)methyl]pyrrolidin-2-one Chemical compound F[C@@H]1CN(CC[C@H]1C1=CC=C(C=C1)O)[C@H]1C(N(CC1)CC1=CC=C(C=C1)C)=O UNVYDSCXINFREZ-BHDDXSALSA-N 0.000 claims 1
- HKJQOALDDUBRBV-UHFFFAOYSA-N 3-[3,3-difluoro-4-(4-hydroxyphenyl)piperidin-1-yl]-1-[(4-methylphenyl)methyl]pyrrolidin-2-one Chemical compound FC1(CN(CCC1C1=CC=C(C=C1)O)C1C(N(CC1)CC1=CC=C(C=C1)C)=O)F HKJQOALDDUBRBV-UHFFFAOYSA-N 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461925363P | 2014-01-09 | 2014-01-09 | |
| US61/925,363 | 2014-01-09 | ||
| PCT/US2015/010262 WO2015105772A1 (en) | 2014-01-09 | 2015-01-06 | Selective nr2b antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017502063A JP2017502063A (ja) | 2017-01-19 |
| JP2017502063A5 true JP2017502063A5 (https=) | 2018-02-08 |
| JP6543259B2 JP6543259B2 (ja) | 2019-07-10 |
Family
ID=52463126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016545819A Expired - Fee Related JP6543259B2 (ja) | 2014-01-09 | 2015-01-06 | 選択的ｎｒ２ｂアンタゴニスト |
Country Status (28)
| Country | Link |
|---|---|
| US (10) | US9221796B2 (https=) |
| EP (1) | EP3092224B1 (https=) |
| JP (1) | JP6543259B2 (https=) |
| KR (1) | KR102311518B1 (https=) |
| CN (1) | CN106061961B (https=) |
| AR (1) | AR099071A1 (https=) |
| AU (1) | AU2015205001A1 (https=) |
| CA (1) | CA2936293A1 (https=) |
| CL (1) | CL2016001763A1 (https=) |
| DK (1) | DK3092224T3 (https=) |
| EA (1) | EA201691413A1 (https=) |
| ES (1) | ES2693250T3 (https=) |
| HR (1) | HRP20181585T1 (https=) |
| HU (1) | HUE041986T2 (https=) |
| IL (1) | IL246599A0 (https=) |
| LT (1) | LT3092224T (https=) |
| MX (1) | MX2016008898A (https=) |
| PE (1) | PE20160933A1 (https=) |
| PL (1) | PL3092224T3 (https=) |
| PT (1) | PT3092224T (https=) |
| RS (1) | RS57830B1 (https=) |
| SG (1) | SG11201605618WA (https=) |
| SI (1) | SI3092224T1 (https=) |
| SM (1) | SMT201800619T1 (https=) |
| TR (1) | TR201815579T4 (https=) |
| TW (1) | TWI640515B (https=) |
| UY (1) | UY35947A (https=) |
| WO (1) | WO2015105772A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9221796B2 (en) * | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
| KR102613179B1 (ko) * | 2015-06-01 | 2023-12-14 | 뤼겐 홀딩스 (케이맨) 리미티드 | Nr2b nmda 수용체 길항제로서의 3,3-디플루오로피페리딘 카바메이트 헤테로사이클릭 화합물 |
| BR112018007181A2 (pt) * | 2015-10-14 | 2018-10-16 | Bristol-Myers Squibb Company | antagonistas de nr2b seletivos |
| KR20180063306A (ko) * | 2015-10-14 | 2018-06-11 | 브리스톨-마이어스 스큅 컴퍼니 | 선택적 nr2b 길항제 |
| US11000526B2 (en) | 2016-11-22 | 2021-05-11 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| 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 |
| 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 |
| WO2025113519A1 (zh) * | 2023-11-28 | 2025-06-05 | 成都地奥制药集团有限公司 | 内酰胺环类化合物及其用途 |
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 |
| WO2000063173A1 (en) | 1999-04-14 | 2000-10-26 | 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 |
| 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 |
| SI1648882T1 (sl) | 2003-06-04 | 2009-02-28 | Merck & Co Inc | 3-fluoro-piperidini kot nmda/nr2b antagonisti |
| WO2005035523A1 (en) | 2003-10-08 | 2005-04-21 | Pfizer Japan Inc. | Fused lactam compounds |
| EP2520567A3 (en) | 2006-02-23 | 2012-12-12 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
| EA201070077A1 (ru) | 2007-06-29 | 2010-08-30 | Эмори Юниверсити | Антагонисты nmda-рецепторов с нейропротективным действием |
| 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 RS RS20181296A patent/RS57830B1/sr unknown
- 2015-01-06 CN CN201580012735.9A patent/CN106061961B/zh not_active Expired - Fee Related
- 2015-01-06 SM SM20180619T patent/SMT201800619T1/it unknown
- 2015-01-06 WO PCT/US2015/010262 patent/WO2015105772A1/en not_active Ceased
- 2015-01-06 EA EA201691413A patent/EA201691413A1/ru unknown
- 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 PE PE2016001107A patent/PE20160933A1/es not_active Application Discontinuation
- 2015-01-06 ES ES15703328.3T patent/ES2693250T3/es active Active
- 2015-01-06 MX MX2016008898A patent/MX2016008898A/es unknown
- 2015-01-06 LT LTEP15703328.3T patent/LT3092224T/lt unknown
- 2015-01-06 HU HUE15703328A patent/HUE041986T2/hu unknown
- 2015-01-06 KR KR1020167021356A patent/KR102311518B1/ko not_active Expired - Fee Related
- 2015-01-06 TR TR2018/15579T patent/TR201815579T4/tr unknown
- 2015-01-06 CA CA2936293A patent/CA2936293A1/en not_active Abandoned
- 2015-01-06 HR HRP20181585TT patent/HRP20181585T1/hr unknown
- 2015-01-06 DK DK15703328.3T patent/DK3092224T3/en active
- 2015-01-06 JP JP2016545819A patent/JP6543259B2/ja not_active Expired - Fee Related
- 2015-01-06 SG SG11201605618WA patent/SG11201605618WA/en unknown
- 2015-01-06 PL PL15703328T patent/PL3092224T3/pl unknown
- 2015-01-06 PT PT15703328T patent/PT3092224T/pt unknown
- 2015-01-06 SI SI201530408T patent/SI3092224T1/sl 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
- 2018-12-19 US US16/225,850 patent/US20190117638A1/en not_active Abandoned
-
2019
- 2019-06-27 US US16/454,831 patent/US20190314358A1/en not_active Abandoned
-
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