CN106715435B - 作为nr2b nmda受体拮抗剂的吡咯并嘧啶衍生物 - Google Patents
作为nr2b nmda受体拮抗剂的吡咯并嘧啶衍生物 Download PDFInfo
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- CN106715435B CN106715435B CN201580049617.5A CN201580049617A CN106715435B CN 106715435 B CN106715435 B CN 106715435B CN 201580049617 A CN201580049617 A CN 201580049617A CN 106715435 B CN106715435 B CN 106715435B
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- 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
- A61K31/495—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
-
- 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
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Psychology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Addiction (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462050692P | 2014-09-15 | 2014-09-15 | |
| US62/050,692 | 2014-09-15 | ||
| PCT/US2015/050267 WO2016044323A1 (en) | 2014-09-15 | 2015-09-15 | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN106715435A CN106715435A (zh) | 2017-05-24 |
| CN106715435B true CN106715435B (zh) | 2019-10-01 |
Family
ID=54293326
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580049617.5A Active CN106715435B (zh) | 2014-09-15 | 2015-09-15 | 作为nr2b nmda受体拮抗剂的吡咯并嘧啶衍生物 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US9567341B2 (enExample) |
| EP (1) | EP3194403B1 (enExample) |
| JP (1) | JP6612331B2 (enExample) |
| KR (1) | KR102569031B1 (enExample) |
| CN (1) | CN106715435B (enExample) |
| AU (1) | AU2015317886A1 (enExample) |
| CA (1) | CA2957898C (enExample) |
| DK (1) | DK3194403T3 (enExample) |
| ES (1) | ES2723436T3 (enExample) |
| IL (1) | IL251027A0 (enExample) |
| MX (1) | MX2017002775A (enExample) |
| RU (1) | RU2017107558A (enExample) |
| SG (1) | SG11201701853YA (enExample) |
| WO (1) | WO2016044323A1 (enExample) |
| ZA (1) | ZA201701069B (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201609741A (zh) | 2014-06-04 | 2016-03-16 | 盧郡控股(開曼)有限公司 | 作為nr2b nmda受體拮抗劑之二氟乙基吡啶衍生物 |
| WO2016044323A1 (en) | 2014-09-15 | 2016-03-24 | 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 |
| MX380424B (es) | 2015-06-01 | 2025-03-12 | Rugen Holdings Cayman Ltd | Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b. |
| US10487055B2 (en) | 2016-06-01 | 2019-11-26 | Rhode Island Board Of Education | Diindole compounds useful in treatment of nervous system disorders |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| ES2897050T3 (es) * | 2017-12-08 | 2022-02-28 | Boehringer Ingelheim Int | Derivados de imidazopiridina y el uso de los mismos como medicamento |
| EP3870292A4 (en) | 2018-10-26 | 2022-11-09 | The Research Foundation for The State University of New York | COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE L-DOPA-INDUCED DYSKINESIA |
| EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
| CN117185897A (zh) * | 2023-08-31 | 2023-12-08 | 上海泰坦科技股份有限公司 | 一种二氟甲基卤苯的合成方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1503793A (zh) * | 2001-02-23 | 2004-06-09 | N-取代的非芳基-杂环nmda/nr2b拮抗剂 | |
| CN101163482A (zh) * | 2005-04-19 | 2008-04-16 | 默克公司 | N-烷基-氮杂环烷基nmda/nr2b拮抗剂 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ296236B6 (cs) | 1995-08-11 | 2006-02-15 | Pfizer Inc. | Trihydrát methansulfonátu (1S,2S)-1-(4-hydroxyfenyl)-2-(4-hydroxy-4-fenylpiperidin-1-yl)-1-propanolu, farmaceutický prostredek a farmaceutická kombinace s jeho obsahem |
| 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 |
| CA2527093C (en) | 2003-06-04 | 2009-10-20 | Merck & Co., Inc. | 3-fluoro-piperidines as nmda/nr2b antagonists |
| US7592360B2 (en) | 2003-06-04 | 2009-09-22 | Merck & Co., Inc. | 3-fluoro-piperidines as NMDA/NR2B antagonists |
| US7452893B2 (en) * | 2003-08-15 | 2008-11-18 | Merck & Co., Inc. | 4-cycloakylaminopyrazolo pyrimidine 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 |
| JP2008525486A (ja) | 2004-12-22 | 2008-07-17 | メルク エンド カムパニー インコーポレーテッド | 置換ピペリジンの製造方法 |
| CA2614907C (en) * | 2005-07-29 | 2012-02-28 | Pfizer Products Inc. | Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis |
| 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 |
| RU2009128693A (ru) | 2006-12-27 | 2011-02-10 | Санофи-Авентис (Fr) | Замещенные производные изохинолина и изохинолинона |
| WO2010015637A1 (en) | 2008-08-06 | 2010-02-11 | Novartis Ag | New antiviral modified nucleosides |
| EP2519241A2 (en) | 2009-12-28 | 2012-11-07 | Afraxis, Inc. | Methods for treating autism |
| CA2794808C (en) | 2010-04-16 | 2019-08-20 | Ac Immune S.A. | 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 |
| EP2582374A4 (en) | 2010-06-16 | 2014-03-19 | Afraxis Holdings Inc | METHOD FOR TREATING NERVOUS ELEMENTS |
| US9737531B2 (en) | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| US20140005188A1 (en) | 2011-03-11 | 2014-01-02 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| DK2713722T3 (en) | 2011-05-31 | 2017-07-03 | Celgene Int Ii Sarl | Newly known GLP-1 receptor stabilizers and modulators |
| AU2013251079B2 (en) | 2012-04-20 | 2017-03-23 | Ucb Pharma S.A. | Methods for treating Parkinson's disease |
| PE20151436A1 (es) | 2013-01-29 | 2015-10-10 | Naurex Inc | Moduladores de receptores nmda de espiro-lactama y sus usos |
| MX2016014581A (es) | 2014-05-06 | 2018-02-16 | Univ Northwestern | Composiciones de compuestos que modulan nmdar. |
| TW201609741A (zh) | 2014-06-04 | 2016-03-16 | 盧郡控股(開曼)有限公司 | 作為nr2b nmda受體拮抗劑之二氟乙基吡啶衍生物 |
| WO2016044323A1 (en) | 2014-09-15 | 2016-03-24 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
| WO2016049048A1 (en) | 2014-09-22 | 2016-03-31 | 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 |
| MX380424B (es) | 2015-06-01 | 2025-03-12 | Rugen Holdings Cayman Ltd | Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b. |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
-
2015
- 2015-09-15 WO PCT/US2015/050267 patent/WO2016044323A1/en not_active Ceased
- 2015-09-15 US US14/855,010 patent/US9567341B2/en active Active
- 2015-09-15 JP JP2017514306A patent/JP6612331B2/ja active Active
- 2015-09-15 MX MX2017002775A patent/MX2017002775A/es unknown
- 2015-09-15 KR KR1020177010056A patent/KR102569031B1/ko active Active
- 2015-09-15 SG SG11201701853YA patent/SG11201701853YA/en unknown
- 2015-09-15 EP EP15779059.3A patent/EP3194403B1/en active Active
- 2015-09-15 CN CN201580049617.5A patent/CN106715435B/zh active Active
- 2015-09-15 CA CA2957898A patent/CA2957898C/en active Active
- 2015-09-15 AU AU2015317886A patent/AU2015317886A1/en not_active Abandoned
- 2015-09-15 DK DK15779059.3T patent/DK3194403T3/en active
- 2015-09-15 ES ES15779059T patent/ES2723436T3/es active Active
- 2015-09-15 RU RU2017107558A patent/RU2017107558A/ru not_active Application Discontinuation
-
2017
- 2017-02-09 US US15/428,321 patent/US9968610B2/en active Active
- 2017-02-13 ZA ZA2017/01069A patent/ZA201701069B/en unknown
- 2017-03-08 IL IL251027A patent/IL251027A0/en unknown
-
2018
- 2018-04-24 US US15/961,553 patent/US10420768B2/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1503793A (zh) * | 2001-02-23 | 2004-06-09 | N-取代的非芳基-杂环nmda/nr2b拮抗剂 | |
| CN101163482A (zh) * | 2005-04-19 | 2008-04-16 | 默克公司 | N-烷基-氮杂环烷基nmda/nr2b拮抗剂 |
Also Published As
| Publication number | Publication date |
|---|---|
| DK3194403T3 (en) | 2019-04-15 |
| US9567341B2 (en) | 2017-02-14 |
| EP3194403A1 (en) | 2017-07-26 |
| US10420768B2 (en) | 2019-09-24 |
| MX2017002775A (es) | 2017-08-10 |
| JP6612331B2 (ja) | 2019-11-27 |
| RU2017107558A (ru) | 2018-10-18 |
| BR112017004868A2 (pt) | 2017-12-12 |
| EP3194403B1 (en) | 2019-02-06 |
| US9968610B2 (en) | 2018-05-15 |
| US20180303834A1 (en) | 2018-10-25 |
| CA2957898C (en) | 2023-02-21 |
| CA2957898A1 (en) | 2016-03-24 |
| ES2723436T3 (es) | 2019-08-27 |
| JP2017526724A (ja) | 2017-09-14 |
| IL251027A0 (en) | 2017-04-30 |
| CN106715435A (zh) | 2017-05-24 |
| RU2017107558A3 (enExample) | 2019-03-18 |
| SG11201701853YA (en) | 2017-04-27 |
| AU2015317886A1 (en) | 2017-03-09 |
| US20160075713A1 (en) | 2016-03-17 |
| WO2016044323A1 (en) | 2016-03-24 |
| KR20170049602A (ko) | 2017-05-10 |
| US20170209449A1 (en) | 2017-07-27 |
| ZA201701069B (en) | 2019-07-31 |
| KR102569031B1 (ko) | 2023-08-22 |
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