ES2723436T3 - Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B - Google Patents
Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B Download PDFInfo
- Publication number
- ES2723436T3 ES2723436T3 ES15779059T ES15779059T ES2723436T3 ES 2723436 T3 ES2723436 T3 ES 2723436T3 ES 15779059 T ES15779059 T ES 15779059T ES 15779059 T ES15779059 T ES 15779059T ES 2723436 T3 ES2723436 T3 ES 2723436T3
- Authority
- ES
- Spain
- Prior art keywords
- fluoro
- optionally substituted
- receptor antagonists
- alkyl
- nr2b receptor
- 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
-
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Physiology (AREA)
- Nutrition Science (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)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Entidad química, que es un compuesto de fórmula I: **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en la que: Y y Z son independientemente N o C(R2); X es -H; halo; alquilo C1-C6 opcionalmente sustituido con de 1 a 6 fluoro; cicloalquilo C3-C6; alcoxilo C3-C4 opcionalmente sustituido con de 1 a 6 fluoro; -CN; -NO2; -N(R7)(R8); -SR7; -S(O)2R9; o -C(O)OR7; R1 es -H; halo; alquilo C1-C4 opcionalmente sustituido con de 1 a 3 fluoro; cicloalquilo C3-C6; alcoxilo C1-C4 opcionalmente sustituido con de 1 a 3 fluoro; -CN; -NO2; -N(R7)(R8); -C(O)OR7; o -C(O)N(R7)(R8); R2 es -H; halo; alquilo C1-C4 opcionalmente sustituido con de 1 a 3 fluoro; ciclopropilo; o alcoxilo C1-C4 opcionalmente sustituido con de 1 a 3 fluoro; R3 es -H, -F, -Cl, -CH3, -CF3 o -OCH3; R4 es -H; -F; -Cl; alquilo C1-C3 opcionalmente sustituido con de 1 a 3 fluoro; o ciclopropilo; R5 es -H o -CH3; R6 es -H, -F o -CH3; cada aparición de R7 es independientemente alquilo C1-C4; cada aparición de R8 es independientemente -H o alquilo C1-C4; y R9 es alquilo C1-C4 opcionalmente sustituido con de 1 a 3 fluoro.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462050692P | 2014-09-15 | 2014-09-15 | |
| PCT/US2015/050267 WO2016044323A1 (en) | 2014-09-15 | 2015-09-15 | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2723436T3 true ES2723436T3 (es) | 2019-08-27 |
Family
ID=54293326
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES15779059T Active ES2723436T3 (es) | 2014-09-15 | 2015-09-15 | Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US9567341B2 (es) |
| EP (1) | EP3194403B1 (es) |
| JP (1) | JP6612331B2 (es) |
| KR (1) | KR102569031B1 (es) |
| CN (1) | CN106715435B (es) |
| AU (1) | AU2015317886A1 (es) |
| CA (1) | CA2957898C (es) |
| DK (1) | DK3194403T3 (es) |
| ES (1) | ES2723436T3 (es) |
| IL (1) | IL251027A0 (es) |
| MX (1) | MX2017002775A (es) |
| RU (1) | RU2017107558A (es) |
| SG (1) | SG11201701853YA (es) |
| WO (1) | WO2016044323A1 (es) |
| ZA (1) | ZA201701069B (es) |
Families Citing this family (8)
| 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 |
| ES2723436T3 (es) | 2014-09-15 | 2019-08-27 | Rugen Holdings Cayman Ltd | Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B |
| WO2016126869A1 (en) | 2015-02-04 | 2016-08-11 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| TWI721987B (zh) | 2015-06-01 | 2021-03-21 | 開曼群島商盧郡控股（開曼）有限公司 | 做為nr2b nmda受體拮抗劑之3,3-二氟哌啶胺基甲酸酯雜環化合物 |
| US10487055B2 (en) | 2016-06-01 | 2019-11-26 | Rhode Island Board Of Education | Diindole compounds useful in treatment of nervous system disorders |
| EP3544610A1 (en) | 2016-11-22 | 2019-10-02 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| HUE056667T2 (hu) * | 2017-12-08 | 2022-02-28 | Boehringer Ingelheim Int | Imidazopiridin-származékok és gyógyszerként történõ alkalmazásuk |
| EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997007098A1 (en) | 1995-08-11 | 1997-02-27 | Pfizer Inc. | (1s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanolmethanesulfonate trihydrate |
| 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 |
| NZ527365A (en) | 2001-02-23 | 2005-08-26 | 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 |
| DK1648882T3 (da) | 2003-06-04 | 2008-11-24 | Merck & Co Inc | 3-fluor-piperidiner som NMDA/NR2B-antagonister |
| EP1656379B1 (en) * | 2003-08-15 | 2007-01-10 | Merck & Co., Inc. | 4-cycloalkylaminopyrazolo 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 |
| AU2005271669A1 (en) * | 2004-08-03 | 2006-02-16 | Merck & Co., Inc. | 1,3-disubstituted heteroaryl NMDA/NR2B antagonists |
| CN101084191A (zh) | 2004-12-22 | 2007-12-05 | 默克公司 | 用于制备取代哌啶类化合物的方法 |
| AU2006236625A1 (en) * | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl NMDA/NR2B antagonists |
| NZ565363A (en) | 2005-07-29 | 2010-03-26 | Pfizer Prod 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 |
| MX2009006517A (es) | 2006-12-27 | 2009-06-26 | Sanofi Aventis | Nuevos derivados de isoquinolina e isoquinolinona sustituidos. |
| WO2010015637A1 (en) | 2008-08-06 | 2010-02-11 | Novartis Ag | New antiviral modified nucleosides |
| US20130096115A1 (en) | 2009-12-28 | 2013-04-18 | 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 |
| 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 |
| JP2014507458A (ja) | 2011-03-11 | 2014-03-27 | グラクソ グループ リミテッド | Ｓｙｋインヒビターとしてのピリド［３，４−Ｂ］ピラジン誘導体 |
| EP2713722B1 (en) | 2011-05-31 | 2017-03-15 | Receptos, LLC | Novel glp-1 receptor stabilizers and modulators |
| JP6042968B2 (ja) | 2012-04-20 | 2016-12-14 | ユセベ ファルマ ソシエテ アノニム | パーキンソン病の処置方法 |
| BR112015018094A2 (pt) | 2013-01-29 | 2017-07-18 | Naurex Inc | moduladores de receptor nmda de espiro-lactama e usos dos mesmos |
| WO2015171770A1 (en) | 2014-05-06 | 2015-11-12 | Northwestern University | Combinations of nmdar modulating compounds |
| 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 |
| ES2723436T3 (es) | 2014-09-15 | 2019-08-27 | Rugen Holdings Cayman Ltd | Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B |
| 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 |
| WO2016126869A1 (en) | 2015-02-04 | 2016-08-11 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| TWI721987B (zh) | 2015-06-01 | 2021-03-21 | 開曼群島商盧郡控股（開曼）有限公司 | 做為nr2b nmda受體拮抗劑之3,3-二氟哌啶胺基甲酸酯雜環化合物 |
| EP3544610A1 (en) | 2016-11-22 | 2019-10-02 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
-
2015
- 2015-09-15 ES ES15779059T patent/ES2723436T3/es active Active
- 2015-09-15 US US14/855,010 patent/US9567341B2/en active Active
- 2015-09-15 AU AU2015317886A patent/AU2015317886A1/en not_active Abandoned
- 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 SG SG11201701853YA patent/SG11201701853YA/en unknown
- 2015-09-15 CA CA2957898A patent/CA2957898C/en active Active
- 2015-09-15 WO PCT/US2015/050267 patent/WO2016044323A1/en active Application Filing
- 2015-09-15 RU RU2017107558A patent/RU2017107558A/ru not_active Application Discontinuation
- 2015-09-15 KR KR1020177010056A patent/KR102569031B1/ko active IP Right Grant
- 2015-09-15 DK DK15779059.3T patent/DK3194403T3/en active
- 2015-09-15 JP JP2017514306A patent/JP6612331B2/ja active Active
- 2015-09-15 MX MX2017002775A patent/MX2017002775A/es unknown
-
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 |
|---|---|
| CA2957898A1 (en) | 2016-03-24 |
| KR102569031B1 (ko) | 2023-08-22 |
| US20170209449A1 (en) | 2017-07-27 |
| RU2017107558A (ru) | 2018-10-18 |
| CA2957898C (en) | 2023-02-21 |
| AU2015317886A1 (en) | 2017-03-09 |
| IL251027A0 (en) | 2017-04-30 |
| DK3194403T3 (en) | 2019-04-15 |
| JP6612331B2 (ja) | 2019-11-27 |
| US9567341B2 (en) | 2017-02-14 |
| WO2016044323A1 (en) | 2016-03-24 |
| US10420768B2 (en) | 2019-09-24 |
| MX2017002775A (es) | 2017-08-10 |
| JP2017526724A (ja) | 2017-09-14 |
| SG11201701853YA (en) | 2017-04-27 |
| RU2017107558A3 (es) | 2019-03-18 |
| EP3194403A1 (en) | 2017-07-26 |
| BR112017004868A2 (pt) | 2017-12-12 |
| US20180303834A1 (en) | 2018-10-25 |
| ZA201701069B (en) | 2019-07-31 |
| CN106715435B (zh) | 2019-10-01 |
| KR20170049602A (ko) | 2017-05-10 |
| CN106715435A (zh) | 2017-05-24 |
| US20160075713A1 (en) | 2016-03-17 |
| US9968610B2 (en) | 2018-05-15 |
| EP3194403B1 (en) | 2019-02-06 |
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