JP6612331B2 - Ｎｒ２ｂ ｎｍｄａ受容体アンタゴニストとしてのピロロピリミジン誘導体 - Google Patents

Ｎｒ２ｂ ｎｍｄａ受容体アンタゴニストとしてのピロロピリミジン誘導体 Download PDF

Info

Publication number
JP6612331B2
JP6612331B2 JP2017514306A JP2017514306A JP6612331B2 JP 6612331 B2 JP6612331 B2 JP 6612331B2 JP 2017514306 A JP2017514306 A JP 2017514306A JP 2017514306 A JP2017514306 A JP 2017514306A JP 6612331 B2 JP6612331 B2 JP 6612331B2
Authority
JP
Japan
Prior art keywords
mmol
formula
epilepsy
chemical entity
difluoro
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.)
Active
Application number
JP2017514306A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017526724A (ja
JP2017526724A5 (enExample
Inventor
ギデオン シャピロ，
Original Assignee
リューゲン ホールディングス （ケイマン） リミテッド
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by リューゲン ホールディングス （ケイマン） リミテッド filed Critical リューゲン ホールディングス （ケイマン） リミテッド
Publication of JP2017526724A publication Critical patent/JP2017526724A/ja
Publication of JP2017526724A5 publication Critical patent/JP2017526724A5/ja
Application granted granted Critical
Publication of JP6612331B2 publication Critical patent/JP6612331B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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)
  • 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)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Addiction (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (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)
JP2017514306A 2014-09-15 2015-09-15 Ｎｒ２ｂ ｎｍｄａ受容体アンタゴニストとしてのピロロピリミジン誘導体 Active JP6612331B2 (ja)

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 (3)

Publication Number Publication Date
JP2017526724A JP2017526724A (ja) 2017-09-14
JP2017526724A5 JP2017526724A5 (enExample) 2018-10-25
JP6612331B2 true JP6612331B2 (ja) 2019-11-27

Family

ID=54293326

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017514306A Active JP6612331B2 (ja) 2014-09-15 2015-09-15 Ｎｒ２ｂ ｎｍｄａ受容体アンタゴニストとしてのピロロピリミジン誘導体

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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (33)

* Cited by examiner, † Cited by third party
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
EA005974B1 (ru) * 2001-02-23 2005-08-25 Мерк Энд Ко., Инк. N-замещенные неарильные гетероциклические антагонисты nmda/nr2b
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
WO2006113471A2 (en) 2005-04-19 2006-10-26 Merck & Co., Inc. N-alkyl-azacycloalkyl nmda/nr2b antagonists
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

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
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
CN106715435B (zh) 2019-10-01
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

Similar Documents

Publication Publication Date Title
JP6612331B2 (ja) Ｎｒ２ｂ ｎｍｄａ受容体アンタゴニストとしてのピロロピリミジン誘導体
KR102189560B1 (ko) Pde4 의 헤테로아릴 저해제
CN106795163B (zh) 作为nr2b nmda受体拮抗剂的二氟乙基吡啶衍生物
JP6876625B2 (ja) Ｎｒ２ｂｎｍｄａレセプターアンタゴニストとしての３，３−ジフルオロピペリジンカルバメート複素環式化合物
WO2016100349A2 (en) Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists
WO2016126869A1 (en) 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
BR112017004868B1 (pt) Derivados de pirrolopirimidina como antagonistas do receptor nmda nr2b e composição farmacêutica que os compreende
HK1241366B (en) Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
HK1241366A1 (en) Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
HK1253023B (en) 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180914

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180914

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190522

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190523

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190709

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20191004

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20191030

R150 Certificate of patent or registration of utility model

Ref document number: 6612331

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250