CA2957898C - Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists - Google Patents
Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists Download PDFInfo
- Publication number
- CA2957898C CA2957898C CA2957898A CA2957898A CA2957898C CA 2957898 C CA2957898 C CA 2957898C CA 2957898 A CA2957898 A CA 2957898A CA 2957898 A CA2957898 A CA 2957898A CA 2957898 C CA2957898 C CA 2957898C
- Authority
- CA
- Canada
- Prior art keywords
- chemical entity
- formula
- mmol
- concentrated
- mixture
- 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.)
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Classifications
-
- 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
-
- 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
Landscapes
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (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 |
|---|---|
| CA2957898A1 CA2957898A1 (en) | 2016-03-24 |
| CA2957898C true CA2957898C (en) | 2023-02-21 |
Family
ID=54293326
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2957898A Active CA2957898C (en) | 2014-09-15 | 2015-09-15 | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
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 |
|---|---|---|---|---|
| US10030026B2 (en) | 2014-06-04 | 2018-07-24 | Rugen Holdings (Cayman) Limited | Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists |
| MX2017002775A (es) | 2014-09-15 | 2017-08-10 | Rugen Holdings (Cayman) Ltd | Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b. |
| US10221182B2 (en) | 2015-02-04 | 2019-03-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists |
| CA2987606C (en) | 2015-06-01 | 2024-02-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists |
| 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 |
| RS62517B1 (sr) * | 2017-12-08 | 2021-11-30 | Boehringer Ingelheim Int | Derivati imidazopiridina i njihova upotreba kao leka |
| 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 |
| 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 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL122649A (en) | 1995-08-11 | 2001-08-26 | Pfizer | (1s, 2s) - 1- (4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol methanesulfonate trihydrate, its use in the preparation of medicaments and pharmaceutical compositions comprising same |
| 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 |
| MXPA03007621A (es) * | 2001-02-23 | 2003-12-04 | Merck & Co Inc | Antagonistas nr2b de n-metil-d-aspartato no arilheterociclicos n-sustituidos. |
| KR20060017839A (ko) | 2003-06-04 | 2006-02-27 | 머크 앤드 캄파니 인코포레이티드 | Nmda/nr2b 길항제로서 3-플루오로-피페리딘 |
| 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 |
| US20070293515A1 (en) | 2004-08-03 | 2007-12-20 | Layton Mark E | 1,3-Disubstituted Heteroaryl Nmda/Nr2b Antagonists |
| CA2591738A1 (en) | 2004-12-22 | 2006-06-29 | Merck & Co., Inc. | Process for making substituted piperidines |
| CA2603876A1 (en) | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl nmda/nr2b antagonists |
| WO2007012953A2 (en) * | 2005-07-29 | 2007-02-01 | 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 |
| KR20090094338A (ko) | 2006-12-27 | 2009-09-04 | 사노피-아벤티스 | 치환된 이소퀴놀린 및 이소퀴놀리논 유도체 |
| 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 |
| ES2734552T3 (es) | 2010-04-16 | 2019-12-10 | Ac Immune Sa | Compuestos novedosos para el tratamiento de enfermedades asociadas a proteínas amiloides o de tipo amiloide |
| US20130231348A1 (en) | 2010-06-09 | 2013-09-05 | Afraxis, 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 |
| US20140005188A1 (en) | 2011-03-11 | 2014-01-02 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| 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 |
| AU2013251079B2 (en) | 2012-04-20 | 2017-03-23 | Ucb Pharma S.A. | Methods for treating Parkinson's disease |
| CN105308049A (zh) | 2013-01-29 | 2016-02-03 | 阿普廷伊克斯股份有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
| BR112016025910A8 (pt) | 2014-05-06 | 2021-07-13 | Univ Northwestern | uso de uma quantidade eficaz de glyx-13, uso de glyx-13 e um antagonista de nmdar e composição farmaceuticamente aceitável compreendendo os mesmos |
| US10030026B2 (en) | 2014-06-04 | 2018-07-24 | Rugen Holdings (Cayman) Limited | Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists |
| MX2017002775A (es) | 2014-09-15 | 2017-08-10 | Rugen Holdings (Cayman) Ltd | Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b. |
| US20180271869A1 (en) | 2014-09-22 | 2018-09-27 | Jie Liu | 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 |
| US10221182B2 (en) | 2015-02-04 | 2019-03-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists |
| CA2987606C (en) | 2015-06-01 | 2024-02-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists |
| 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 MX MX2017002775A patent/MX2017002775A/es unknown
- 2015-09-15 SG SG11201701853YA patent/SG11201701853YA/en unknown
- 2015-09-15 JP JP2017514306A patent/JP6612331B2/ja active Active
- 2015-09-15 WO PCT/US2015/050267 patent/WO2016044323A1/en not_active Ceased
- 2015-09-15 CN CN201580049617.5A patent/CN106715435B/zh active Active
- 2015-09-15 KR KR1020177010056A patent/KR102569031B1/ko active Active
- 2015-09-15 RU RU2017107558A patent/RU2017107558A/ru not_active Application Discontinuation
- 2015-09-15 ES ES15779059T patent/ES2723436T3/es active Active
- 2015-09-15 DK DK15779059.3T patent/DK3194403T3/en active
- 2015-09-15 US US14/855,010 patent/US9567341B2/en active Active
- 2015-09-15 EP EP15779059.3A patent/EP3194403B1/en active Active
- 2015-09-15 CA CA2957898A patent/CA2957898C/en active Active
- 2015-09-15 AU AU2015317886A patent/AU2015317886A1/en not_active Abandoned
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| RU2017107558A3 (enExample) | 2019-03-18 |
| IL251027A0 (en) | 2017-04-30 |
| KR102569031B1 (ko) | 2023-08-22 |
| CN106715435A (zh) | 2017-05-24 |
| CA2957898A1 (en) | 2016-03-24 |
| AU2015317886A1 (en) | 2017-03-09 |
| ES2723436T3 (es) | 2019-08-27 |
| KR20170049602A (ko) | 2017-05-10 |
| US20180303834A1 (en) | 2018-10-25 |
| US20160075713A1 (en) | 2016-03-17 |
| SG11201701853YA (en) | 2017-04-27 |
| US20170209449A1 (en) | 2017-07-27 |
| MX2017002775A (es) | 2017-08-10 |
| DK3194403T3 (en) | 2019-04-15 |
| US9567341B2 (en) | 2017-02-14 |
| WO2016044323A1 (en) | 2016-03-24 |
| EP3194403B1 (en) | 2019-02-06 |
| US10420768B2 (en) | 2019-09-24 |
| ZA201701069B (en) | 2019-07-31 |
| CN106715435B (zh) | 2019-10-01 |
| JP6612331B2 (ja) | 2019-11-27 |
| BR112017004868A2 (pt) | 2017-12-12 |
| JP2017526724A (ja) | 2017-09-14 |
| RU2017107558A (ru) | 2018-10-18 |
| US9968610B2 (en) | 2018-05-15 |
| EP3194403A1 (en) | 2017-07-26 |
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