KR102569031B1 - Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체 - Google Patents

Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체 Download PDF

Info

Publication number
KR102569031B1
KR102569031B1 KR1020177010056A KR20177010056A KR102569031B1 KR 102569031 B1 KR102569031 B1 KR 102569031B1 KR 1020177010056 A KR1020177010056 A KR 1020177010056A KR 20177010056 A KR20177010056 A KR 20177010056A KR 102569031 B1 KR102569031 B1 KR 102569031B1
Authority
KR
South Korea
Prior art keywords
formula
mmol
difluoro
ethyl
concentrated
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
KR1020177010056A
Other languages
English (en)
Korean (ko)
Other versions
KR20170049602A (ko
Inventor
기디언 샤피로
Original Assignee
뤼겐 홀딩스 (케이맨) 리미티드
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 뤼겐 홀딩스 (케이맨) 리미티드 filed Critical 뤼겐 홀딩스 (케이맨) 리미티드
Publication of KR20170049602A publication Critical patent/KR20170049602A/ko
Application granted granted Critical
Publication of KR102569031B1 publication Critical patent/KR102569031B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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)
  • 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)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (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)
KR1020177010056A 2014-09-15 2015-09-15 Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체 Active KR102569031B1 (ko)

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
KR20170049602A KR20170049602A (ko) 2017-05-10
KR102569031B1 true KR102569031B1 (ko) 2023-08-22

Family

ID=54293326

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177010056A Active KR102569031B1 (ko) 2014-09-15 2015-09-15 Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체

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
CN106795163B (zh) 2014-06-04 2019-07-30 卢郡控股(开曼)有限公司 作为nr2b nmda受体拮抗剂的二氟乙基吡啶衍生物
KR102569031B1 (ko) 2014-09-15 2023-08-22 뤼겐 홀딩스 (케이맨) 리미티드 Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체
EP3253761A4 (en) 2015-02-04 2018-06-20 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
WO2016196513A1 (en) 2015-06-01 2016-12-08 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
HRP20211726T1 (hr) * 2017-12-08 2022-02-18 Boehringer Ingelheim International Gmbh Derivati imidazopiridina i njihova uporaba kao lijeka
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004524314A (ja) 2001-02-23 2004-08-12 メルク　エンド　カムパニー　インコーポレーテッド Ｎ−置換非アリール系複素環ｎｍｄａ／ｎｒ２ｂ拮抗薬
JP2007502772A (ja) 2003-08-15 2007-02-15 メルク　エンド　カムパニー　インコーポレーテッド ４−シクロアルキルアミノピラゾロピリミジンｎｍｄａ／ｎｒ２ｂ拮抗薬
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
JP2008536927A (ja) 2005-04-19 2008-09-11 メルク エンド カムパニー インコーポレーテッド Ｎ−アルキル−アザシクロアルキルｎｍｄａ／ｎｒ２ｂ拮抗物質
US20120259115A1 (en) 2005-07-29 2012-10-11 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2170857T3 (es) 1995-08-11 2002-08-16 Pfizer Metanosulfonato de (1s,2s)-1-(4-hidroxifenil)-2-(4-hidroxi-4-fenilpiperidin-1-il)-1-propanol trihidrato.
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
MXPA05013151A (es) 2003-06-04 2006-03-17 Merck & Co Inc 3-fluoro-piperidinas como antagonistas de n-metil-d-aspartato/nr2b.
US7592360B2 (en) 2003-06-04 2009-09-22 Merck & Co., Inc. 3-fluoro-piperidines as NMDA/NR2B antagonists
WO2005102390A2 (en) 2004-04-22 2005-11-03 Pfizer Japan, Inc. Combinations comprising alpha-2-delta ligands and nmda receptor antagonists
WO2006069287A1 (en) 2004-12-22 2006-06-29 Merck & Co., Inc. Process for making substituted piperidines
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
US7935706B2 (en) 2006-02-23 2011-05-03 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
WO2011090666A2 (en) 2009-12-28 2011-07-28 Afraxis, Inc. Methods for treating autism
MY173699A (en) 2010-04-16 2020-02-17 Ac Immune Sa Novel compounds for the treatment of diseases associated with amyloid of amyloid-like proteins
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
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
US20140005188A1 (en) 2011-03-11 2014-01-02 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
EP2713722B1 (en) 2011-05-31 2017-03-15 Receptos, LLC Novel glp-1 receptor stabilizers and modulators
CA2869216A1 (en) 2012-04-20 2013-10-24 Ucb Pharma S.A. Methods for treating parkinson's disease
KR20150110784A (ko) 2013-01-29 2015-10-02 노렉스, 인크. 스피로-락탐 nmda 수용체 조절인자 및 그의 용도
JP2017514871A (ja) 2014-05-06 2017-06-08 ノースウェスタン ユニバーシティ Ｎｍｄａｒ調節化合物の組合せ
CN106795163B (zh) 2014-06-04 2019-07-30 卢郡控股(开曼)有限公司 作为nr2b nmda受体拮抗剂的二氟乙基吡啶衍生物
KR102569031B1 (ko) 2014-09-15 2023-08-22 뤼겐 홀딩스 (케이맨) 리미티드 Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체
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
WO2016196513A1 (en) 2015-06-01 2016-12-08 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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004524314A (ja) 2001-02-23 2004-08-12 メルク　エンド　カムパニー　インコーポレーテッド Ｎ−置換非アリール系複素環ｎｍｄａ／ｎｒ２ｂ拮抗薬
JP2007502772A (ja) 2003-08-15 2007-02-15 メルク　エンド　カムパニー　インコーポレーテッド ４−シクロアルキルアミノピラゾロピリミジンｎｍｄａ／ｎｒ２ｂ拮抗薬
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
JP2008536927A (ja) 2005-04-19 2008-09-11 メルク エンド カムパニー インコーポレーテッド Ｎ−アルキル−アザシクロアルキルｎｍｄａ／ｎｒ２ｂ拮抗物質
US20120259115A1 (en) 2005-07-29 2012-10-11 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis

Also Published As

Publication number Publication date
US9567341B2 (en) 2017-02-14
US20170209449A1 (en) 2017-07-27
WO2016044323A1 (en) 2016-03-24
CA2957898C (en) 2023-02-21
ZA201701069B (en) 2019-07-31
IL251027A0 (en) 2017-04-30
KR20170049602A (ko) 2017-05-10
CN106715435A (zh) 2017-05-24
US20160075713A1 (en) 2016-03-17
AU2015317886A1 (en) 2017-03-09
US20180303834A1 (en) 2018-10-25
ES2723436T3 (es) 2019-08-27
SG11201701853YA (en) 2017-04-27
DK3194403T3 (en) 2019-04-15
BR112017004868A2 (pt) 2017-12-12
MX2017002775A (es) 2017-08-10
EP3194403B1 (en) 2019-02-06
JP6612331B2 (ja) 2019-11-27
JP2017526724A (ja) 2017-09-14
CA2957898A1 (en) 2016-03-24
US9968610B2 (en) 2018-05-15
RU2017107558A (ru) 2018-10-18
EP3194403A1 (en) 2017-07-26
RU2017107558A3 (enExample) 2019-03-18
US10420768B2 (en) 2019-09-24
CN106715435B (zh) 2019-10-01

Similar Documents

Publication Publication Date Title
KR102569031B1 (ko) Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체
US11136328B2 (en) 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
EP3152213B1 (en) Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists
EP3253761A1 (en) 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
TW202033520A (zh) 用作fgfr4抑制劑的稠環衍生物
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
PA0105 International application

Patent event date: 20170413

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20200915

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20221024

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20230516

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20230817

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20230818

End annual number: 3

Start annual number: 1

PG1601 Publication of registration