MX2017002775A - Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b. - Google Patents
Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b.Info
- Publication number
- MX2017002775A MX2017002775A MX2017002775A MX2017002775A MX2017002775A MX 2017002775 A MX2017002775 A MX 2017002775A MX 2017002775 A MX2017002775 A MX 2017002775A MX 2017002775 A MX2017002775 A MX 2017002775A MX 2017002775 A MX2017002775 A MX 2017002775A
- Authority
- MX
- Mexico
- Prior art keywords
- receptor antagonists
- formula
- nmda receptor
- nr2b
- pyrrolopyrimidine derivatives
- Prior art date
Links
- 229940127523 NMDA Receptor Antagonists Drugs 0.000 title 1
- 108010054200 NR2B NMDA receptor Proteins 0.000 title 1
- 150000004944 pyrrolopyrimidines Chemical class 0.000 title 1
- 150000005829 chemical entities Chemical class 0.000 abstract 3
- 102000034527 Retinoid X Receptors Human genes 0.000 abstract 2
- 108010038912 Retinoid X Receptors Proteins 0.000 abstract 2
- 208000037765 diseases and disorders Diseases 0.000 abstract 2
- 230000008485 antagonism Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
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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)
- 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
Se describen las entidades químicas de la fórmula I: (ver Fórmula) en donde X, Y, Z, R1, R3, R4, R5 y R6 son como se definen en la presente, como antagonistas del receptor selectivo del subtipo NR2B. También se describen las composiciones farmacéuticas que comprenden una entidad química de la fórmula I, y los métodos de tratamiento de diversas enfermedades y trastornos asociados con el antagonismo de NR2N, por ejemplo, enfermedades y trastornos del sistema nervioso central, tales como la depresión, por administración de una entidad química de la fórmula I.
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 |
|---|---|
| MX2017002775A true MX2017002775A (es) | 2017-08-10 |
Family
ID=54293326
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017002775A MX2017002775A (es) | 2014-09-15 | 2015-09-15 | Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad 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 (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3152213B1 (en) * | 2014-06-04 | 2018-10-31 | Rugen Holdings (Cayman) Limited | Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists |
| EP3194403B1 (en) | 2014-09-15 | 2019-02-06 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives 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 |
| US10584127B2 (en) | 2015-06-01 | 2020-03-10 | 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 |
| US11000526B2 (en) | 2016-11-22 | 2021-05-11 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| SG11202005138TA (en) * | 2017-12-08 | 2020-06-29 | Boehringer Ingelheim Int | Imidazopyridine derivatives and the use thereof as medicament |
| WO2020087031A1 (en) | 2018-10-26 | 2020-04-30 | 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 |
|---|---|---|---|---|
| EP0843661B1 (en) | 1995-08-11 | 2002-03-27 | 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 |
| PT1379520E (pt) | 2001-02-23 | 2006-08-31 | Merck & Co Inc | Antagonistas (nao-aril)-heterociclicos n-substituidos de nmda/nr2b |
| US7592360B2 (en) | 2003-06-04 | 2009-09-22 | Merck & Co., Inc. | 3-fluoro-piperidines as NMDA/NR2B antagonists |
| MXPA05013151A (es) | 2003-06-04 | 2006-03-17 | Merck & Co Inc | 3-fluoro-piperidinas como antagonistas de n-metil-d-aspartato/nr2b. |
| CN1835953A (zh) | 2003-08-15 | 2006-09-20 | 默克专利 | 4－环烷基氨基吡唑并嘧啶nmda/nr2b拮抗剂 |
| WO2005102390A2 (en) | 2004-04-22 | 2005-11-03 | Pfizer Japan, Inc. | Combinations comprising alpha-2-delta ligands and nmda receptor antagonists |
| JP2008509139A (ja) | 2004-08-03 | 2008-03-27 | メルク エンド カムパニー インコーポレーテッド | １，３−二置換ヘテロアリールｎｍｄａ／ｎｒ２ｂ拮抗薬 |
| US20080086006A1 (en) | 2004-12-22 | 2008-04-10 | Nelson Todd D | Process for Making Substituted Piperidines |
| WO2006113471A2 (en) * | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl nmda/nr2b antagonists |
| RU2384583C2 (ru) | 2005-07-29 | 2010-03-20 | Пфайзер Продактс Инк. | ПИРРОЛО[2,3-d]ПИРИМИДИНОВЫЕ ПРОИЗВОДНЫЕ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ И СИНТЕЗ |
| 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 |
| JPWO2007099828A1 (ja) | 2006-02-23 | 2009-07-16 | 塩野義製薬株式会社 | 環式基で置換された含窒素複素環誘導体 |
| 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 |
| KR101851810B1 (ko) | 2010-04-16 | 2018-04-26 | 에이씨 이뮨 에스.에이. | 아밀로이드 또는 아밀로이드-유사 단백질과 관련된 질환의 치료를 위한 신규 화합물 |
| WO2011156640A2 (en) | 2010-06-09 | 2011-12-15 | Afraxis, Inc. | 8-(HETEROARYLMETHYL)PYRIDO[2,3-d]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS |
| US20130225575A1 (en) | 2010-06-16 | 2013-08-29 | 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 |
| DK2713722T3 (en) | 2011-05-31 | 2017-07-03 | Celgene Int Ii Sarl | Newly known GLP-1 receptor stabilizers and modulators |
| EP2838530B1 (en) | 2012-04-20 | 2017-04-05 | UCB Biopharma SPRL | Methods for treating parkinson's disease |
| SG11201505862TA (en) | 2013-01-29 | 2015-08-28 | Naurex Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| CN106659762A (zh) | 2014-05-06 | 2017-05-10 | 西北大学 | Nmdar调节化合物的组合 |
| EP3152213B1 (en) | 2014-06-04 | 2018-10-31 | Rugen Holdings (Cayman) Limited | Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists |
| EP3194403B1 (en) | 2014-09-15 | 2019-02-06 | 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 |
| US10221182B2 (en) | 2015-02-04 | 2019-03-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists |
| US10584127B2 (en) | 2015-06-01 | 2020-03-10 | Rugen Holdings (Cayman) Limited | 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists |
| US11000526B2 (en) | 2016-11-22 | 2021-05-11 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
-
2015
- 2015-09-15 EP EP15779059.3A patent/EP3194403B1/en active Active
- 2015-09-15 SG SG11201701853YA patent/SG11201701853YA/en unknown
- 2015-09-15 DK DK15779059.3T patent/DK3194403T3/en active
- 2015-09-15 AU AU2015317886A patent/AU2015317886A1/en not_active Abandoned
- 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 MX MX2017002775A patent/MX2017002775A/es unknown
- 2015-09-15 KR KR1020177010056A patent/KR102569031B1/ko active Active
- 2015-09-15 CA CA2957898A patent/CA2957898C/en active Active
- 2015-09-15 CN CN201580049617.5A patent/CN106715435B/zh active Active
- 2015-09-15 RU RU2017107558A patent/RU2017107558A/ru not_active Application Discontinuation
- 2015-09-15 WO PCT/US2015/050267 patent/WO2016044323A1/en not_active Ceased
- 2015-09-15 JP JP2017514306A patent/JP6612331B2/ja active Active
-
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 |
|---|---|
| CN106715435B (zh) | 2019-10-01 |
| SG11201701853YA (en) | 2017-04-27 |
| ZA201701069B (en) | 2019-07-31 |
| US20170209449A1 (en) | 2017-07-27 |
| US9968610B2 (en) | 2018-05-15 |
| BR112017004868A2 (pt) | 2017-12-12 |
| EP3194403B1 (en) | 2019-02-06 |
| KR102569031B1 (ko) | 2023-08-22 |
| ES2723436T3 (es) | 2019-08-27 |
| US20180303834A1 (en) | 2018-10-25 |
| IL251027A0 (en) | 2017-04-30 |
| EP3194403A1 (en) | 2017-07-26 |
| JP6612331B2 (ja) | 2019-11-27 |
| US20160075713A1 (en) | 2016-03-17 |
| CA2957898A1 (en) | 2016-03-24 |
| WO2016044323A1 (en) | 2016-03-24 |
| DK3194403T3 (en) | 2019-04-15 |
| US9567341B2 (en) | 2017-02-14 |
| CN106715435A (zh) | 2017-05-24 |
| KR20170049602A (ko) | 2017-05-10 |
| CA2957898C (en) | 2023-02-21 |
| AU2015317886A1 (en) | 2017-03-09 |
| RU2017107558A (ru) | 2018-10-18 |
| RU2017107558A3 (es) | 2019-03-18 |
| JP2017526724A (ja) | 2017-09-14 |
| US10420768B2 (en) | 2019-09-24 |
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