CN107849010B - 作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物 - Google Patents
作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物 Download PDFInfo
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- CN107849010B CN107849010B CN201680042502.8A CN201680042502A CN107849010B CN 107849010 B CN107849010 B CN 107849010B CN 201680042502 A CN201680042502 A CN 201680042502A CN 107849010 B CN107849010 B CN 107849010B
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- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562169107P | 2015-06-01 | 2015-06-01 | |
| US62/169,107 | 2015-06-01 | ||
| PCT/US2016/035098 WO2016196513A1 (en) | 2015-06-01 | 2016-05-31 | 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107849010A CN107849010A (zh) | 2018-03-27 |
| CN107849010B true CN107849010B (zh) | 2021-11-09 |
Family
ID=57441824
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680042502.8A Active CN107849010B (zh) | 2015-06-01 | 2016-05-31 | 作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10584127B2 (https=) |
| EP (1) | EP3303323B1 (https=) |
| JP (1) | JP6876625B2 (https=) |
| KR (1) | KR102613179B1 (https=) |
| CN (1) | CN107849010B (https=) |
| AR (1) | AR104837A1 (https=) |
| AU (1) | AU2016270677B2 (https=) |
| BR (1) | BR112017025023B1 (https=) |
| CA (1) | CA2987606C (https=) |
| DK (1) | DK3303323T3 (https=) |
| ES (1) | ES2784398T3 (https=) |
| IL (1) | IL255937B (https=) |
| MX (1) | MX380424B (https=) |
| RU (1) | RU2735277C2 (https=) |
| TW (1) | TWI721987B (https=) |
| WO (1) | WO2016196513A1 (https=) |
| ZA (1) | ZA201708006B (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015317886A1 (en) | 2014-09-15 | 2017-03-09 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as NR2B NMDA receptor antagonists |
| EP3253761A4 (en) | 2015-02-04 | 2018-06-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| BR112017025023B1 (pt) | 2015-06-01 | 2024-01-30 | Rugen Holdings (Cayman) Limited | Compostos heterocíclicos de carbamato de 3,3-difluoropiperidina, seu uso como antagonistas do receptor nmda nr2b e composição farmacêutica que os compreende |
| CN106986874B (zh) * | 2016-01-20 | 2019-09-24 | 西华大学 | (1H-吡唑[3,4-d]嘧啶)-4-氨基衍生物及其作为IDO抑制剂在药物制备中的用途 |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
| MX2022013029A (es) | 2020-04-17 | 2023-01-16 | Honeybrains Llc | Composiciones y metodos para el tratamiento de trastornos neuropsiquiatricos. |
| CN117159541A (zh) * | 2023-09-20 | 2023-12-05 | 南华大学 | Nat10拮抗剂在制备预防和/或治疗癫痫的药物中的应用 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1798744A (zh) * | 2003-06-04 | 2006-07-05 | 麦克公司 | 作为nmda/nr2b拮抗剂的3-氟-哌啶化合物 |
| WO2012123312A1 (en) * | 2011-03-11 | 2012-09-20 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| WO2013156614A1 (en) * | 2012-04-20 | 2013-10-24 | Ucb Pharma S.A. | Methods for treating parkinson's disease |
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| DE3717867A1 (de) | 1987-05-26 | 1988-12-15 | Schiepe Stapelautomaten Gmbh | Stapelvorrichtung |
| NZ309134A (en) | 1995-08-11 | 1999-09-29 | Pfizer | (1s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1- propranolmethanesulfonate trihydrate |
| GB9805977D0 (en) * | 1998-03-19 | 1998-05-20 | Silver Joshua D | Improvements in variable focus optical devices |
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| HU227197B1 (en) | 2000-10-24 | 2010-10-28 | Richter Gedeon Nyrt | Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them |
| PL364625A1 (en) | 2001-02-23 | 2004-12-13 | Merck & Co, Inc. | N-substituted nonaryl-heterocyclic nmda/nr2b antagonists |
| US7592360B2 (en) | 2003-06-04 | 2009-09-22 | Merck & Co., Inc. | 3-fluoro-piperidines as NMDA/NR2B antagonists |
| WO2005102390A2 (en) | 2004-04-22 | 2005-11-03 | Pfizer Japan, Inc. | Combinations comprising alpha-2-delta ligands and nmda receptor antagonists |
| CN1993363A (zh) | 2004-08-03 | 2007-07-04 | 默克公司 | 1,3-二取代的杂芳基nmda/nr2b拮抗剂 |
| US20080086006A1 (en) * | 2004-12-22 | 2008-04-10 | Nelson Todd D | Process for Making Substituted Piperidines |
| AU2006236625A1 (en) | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl NMDA/NR2B antagonists |
| WO2007061868A2 (en) | 2005-11-17 | 2007-05-31 | Trustees Of Tufts College | Treatment of stereotypic, self-injurious and compulsive behaviors using specific serotonin reuptake inhibitors and antagonists of nmda receptors |
| EP2520567A3 (en) | 2006-02-23 | 2012-12-12 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
| CA2662702A1 (en) * | 2006-09-07 | 2008-03-13 | Merck & Co., Inc. | Difluorinated piperidines for treatment of alzheimer's disease and related conditions |
| EP2114920A1 (en) | 2006-12-27 | 2009-11-11 | Sanofi-Aventis | Substituted isoquinoline and isoquinolinone derivatives |
| WO2009118187A1 (en) | 2008-03-27 | 2009-10-01 | Evotec Neurosciences Gmbh | Methods for treating disorders using nmda nr2b-subtype selective antagonist |
| US20100010565A1 (en) * | 2008-07-09 | 2010-01-14 | Samuel Victor Lichtenstein | Extended range wireless muscular and neural stimulation |
| WO2010015637A1 (en) | 2008-08-06 | 2010-02-11 | Novartis Ag | New antiviral modified nucleosides |
| WO2011090666A2 (en) | 2009-12-28 | 2011-07-28 | Afraxis, Inc. | Methods for treating autism |
| PH12012502079A1 (en) * | 2010-04-16 | 2013-02-11 | Ac Immune Sa | Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
| EP2580213A4 (en) | 2010-06-09 | 2013-12-25 | Afraxis Holdings Inc | 8- (HETEROARYLMETHYL) PYRIDO [2,3-D] PYRIMIDIN-7 (8H) -ONES FOR THE TREATMENT OF CNS DISORDERS |
| WO2011159945A2 (en) | 2010-06-16 | 2011-12-22 | Afraxis, Inc. | Methods for treating neurological conditions |
| US9737531B2 (en) | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| JP6007417B2 (ja) * | 2011-05-31 | 2016-10-12 | レセプトス エルエルシー | 新規glp−1受容体安定剤および調節剤 |
| PE20151162A1 (es) * | 2012-12-11 | 2015-08-28 | Takeda Pharmaceutical | Compuestos heterociclicos inhibidores del colesterol 24-hidroxilasa (ch24h) |
| SG11201505862TA (en) | 2013-01-29 | 2015-08-28 | Naurex Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| CN105849097A (zh) * | 2013-11-06 | 2016-08-10 | 百时美施贵宝公司 | 取代的吡啶衍生物用作gsk-3抑制剂 |
| US9221796B2 (en) * | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
| KR20170013890A (ko) | 2014-05-06 | 2017-02-07 | 노쓰웨스턴유니버시티 | Nmdar 조절 화합물의 조합물 |
| EP3152213B1 (en) | 2014-06-04 | 2018-10-31 | Rugen Holdings (Cayman) Limited | Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists |
| AU2015317886A1 (en) | 2014-09-15 | 2017-03-09 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as NR2B NMDA receptor antagonists |
| EP3197440A4 (en) | 2014-09-22 | 2018-04-18 | Rugen Holdings (Cayman) Limited | Treatment of anxiety disorders and autism spectrum disorders |
| WO2016100349A2 (en) | 2014-12-16 | 2016-06-23 | Rugen Holdings (Cayman) Limited | Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists |
| EP3253761A4 (en) | 2015-02-04 | 2018-06-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| BR112017025023B1 (pt) | 2015-06-01 | 2024-01-30 | Rugen Holdings (Cayman) Limited | Compostos heterocíclicos de carbamato de 3,3-difluoropiperidina, seu uso como antagonistas do receptor nmda nr2b e composição farmacêutica que os compreende |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
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2016
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- 2016-05-31 MX MX2017015370A patent/MX380424B/es unknown
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- 2016-05-31 DK DK16804257.0T patent/DK3303323T3/da active
- 2016-05-31 WO PCT/US2016/035098 patent/WO2016196513A1/en not_active Ceased
- 2016-05-31 US US15/578,460 patent/US10584127B2/en active Active
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- 2016-05-31 ES ES16804257T patent/ES2784398T3/es active Active
- 2016-05-31 CN CN201680042502.8A patent/CN107849010B/zh active Active
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2017
- 2017-11-24 ZA ZA2017/08006A patent/ZA201708006B/en unknown
- 2017-11-27 IL IL255937A patent/IL255937B/en active IP Right Grant
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2018
- 2018-08-10 US US16/100,596 patent/US10294230B2/en active Active
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2020
- 2020-03-05 US US16/810,258 patent/US11136328B2/en active Active
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2021
- 2021-10-01 US US17/491,676 patent/US20220024937A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1798744A (zh) * | 2003-06-04 | 2006-07-05 | 麦克公司 | 作为nmda/nr2b拮抗剂的3-氟-哌啶化合物 |
| WO2012123312A1 (en) * | 2011-03-11 | 2012-09-20 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| WO2013156614A1 (en) * | 2012-04-20 | 2013-10-24 | Ucb Pharma S.A. | Methods for treating parkinson's disease |
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