CN106061961B - 选择性nr2b拮抗剂 - Google Patents

选择性nr2b拮抗剂 Download PDF

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Publication number
CN106061961B
CN106061961B CN201580012735.9A CN201580012735A CN106061961B CN 106061961 B CN106061961 B CN 106061961B CN 201580012735 A CN201580012735 A CN 201580012735A CN 106061961 B CN106061961 B CN 106061961B
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CN
China
Prior art keywords
fluoro
piperidin
hydroxyphenyl
pyrrolidin
mmol
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.)
Expired - Fee Related
Application number
CN201580012735.9A
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English (en)
Chinese (zh)
Other versions
CN106061961A (zh
Inventor
D.金
L.A.汤普森三世
施建良
S.桑加蒂鲁帕蒂
J.S.瓦里尔
I.伊斯拉姆
J.E.马科
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication of CN106061961A publication Critical patent/CN106061961A/zh
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Expired - Fee Related legal-status Critical Current
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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201580012735.9A 2014-01-09 2015-01-06 选择性nr2b拮抗剂 Expired - Fee Related CN106061961B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461925363P 2014-01-09 2014-01-09
US61/925363 2014-01-09
PCT/US2015/010262 WO2015105772A1 (en) 2014-01-09 2015-01-06 Selective nr2b antagonists

Publications (2)

Publication Number Publication Date
CN106061961A CN106061961A (zh) 2016-10-26
CN106061961B true CN106061961B (zh) 2018-12-18

Family

ID=52463126

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580012735.9A Expired - Fee Related CN106061961B (zh) 2014-01-09 2015-01-06 选择性nr2b拮抗剂

Country Status (28)

Country Link
US (10) US9221796B2 (https=)
EP (1) EP3092224B1 (https=)
JP (1) JP6543259B2 (https=)
KR (1) KR102311518B1 (https=)
CN (1) CN106061961B (https=)
AR (1) AR099071A1 (https=)
AU (1) AU2015205001A1 (https=)
CA (1) CA2936293A1 (https=)
CL (1) CL2016001763A1 (https=)
DK (1) DK3092224T3 (https=)
EA (1) EA201691413A1 (https=)
ES (1) ES2693250T3 (https=)
HR (1) HRP20181585T1 (https=)
HU (1) HUE041986T2 (https=)
IL (1) IL246599A0 (https=)
LT (1) LT3092224T (https=)
MX (1) MX2016008898A (https=)
PE (1) PE20160933A1 (https=)
PL (1) PL3092224T3 (https=)
PT (1) PT3092224T (https=)
RS (1) RS57830B1 (https=)
SG (1) SG11201605618WA (https=)
SI (1) SI3092224T1 (https=)
SM (1) SMT201800619T1 (https=)
TR (1) TR201815579T4 (https=)
TW (1) TWI640515B (https=)
UY (1) UY35947A (https=)
WO (1) WO2015105772A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9221796B2 (en) * 2014-01-09 2015-12-29 Bristol-Myers Squibb Company Selective NR2B antagonists
BR112017025023B1 (pt) * 2015-06-01 2024-01-30 Rugen Holdings (Cayman) Limited Compostos heterocíclicos de carbamato de 3,3-difluoropiperidina, seu uso como antagonistas do receptor nmda nr2b e composição farmacêutica que os compreende
ES2822830T3 (es) 2015-10-14 2021-05-05 Bristol Myers Squibb Co Antagonistas selectivos de NR2B
JP6938485B2 (ja) * 2015-10-14 2021-09-22 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 選択的ｎｒ２ｂアンタゴニスト
WO2018098128A1 (en) 2016-11-22 2018-05-31 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
CN108203404A (zh) * 2018-03-02 2018-06-26 上海博邦医药科技有限公司 (r)-3-苯基哌啶或/和(s)-3-苯基哌啶以及尼拉帕尼的手性中间体的合成方法
US10781172B2 (en) 2018-06-21 2020-09-22 Northwestern University Catalysts and methods for enantioselective conjugate additions of amines to unsaturated electrophiles
WO2024197289A1 (en) * 2023-03-22 2024-09-26 Gilgamesh Pharmaceuticals, Inc. Negative allosteric modulators of glun2b receptors and methods of making and using the same
WO2025113519A1 (zh) * 2023-11-28 2025-06-05 成都地奥制药集团有限公司 内酰胺环类化合物及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1441773A (zh) * 2000-04-26 2003-09-10 沃尼尔·朗伯公司 作为亚型选择性nmda受体拮抗剂的环己胺衍生物
CN101815518A (zh) * 2007-06-29 2010-08-25 埃莫里大学 用于神经保护的nmda受体拮抗剂

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2744448B1 (fr) 1996-02-02 1998-04-24 Pf Medicament Nouvelles piperidines derivees d'aryl piperazine, ainsi que leur procede de preparation, les compositions pharmaceutiques et leur utilisation comme medicaments
AU3818900A (en) 1999-04-14 2000-11-02 F. Hoffmann-La Roche Ag Process for the preparation of substituted piperidines
US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
JPWO2003035641A1 (ja) 2001-10-22 2005-02-10 塩野義製薬株式会社 新規カルバモイルピロリドン誘導体
DE602004015610D1 (de) 2003-06-04 2008-09-18 Merck & Co Inc 3-fluoro-piperidine als nmda/nr2b antagonisten
MXPA06003748A (es) 2003-10-08 2006-06-14 Pfizer Compuestos de lactama condensada.
EP2520567A3 (en) 2006-02-23 2012-12-12 Shionogi & Co., Ltd. Nitrogen-containing heterocycle derivatives substituted with cyclic group
US9221796B2 (en) * 2014-01-09 2015-12-29 Bristol-Myers Squibb Company Selective NR2B antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1441773A (zh) * 2000-04-26 2003-09-10 沃尼尔·朗伯公司 作为亚型选择性nmda受体拮抗剂的环己胺衍生物
CN101815518A (zh) * 2007-06-29 2010-08-25 埃莫里大学 用于神经保护的nmda受体拮抗剂

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
1385072-30-9;ACS;《Registry》;20120801 *
1623322-96-2;ACS;《Registry》;20140918 *

Also Published As

Publication number Publication date
PE20160933A1 (es) 2016-09-10
HUE041986T2 (hu) 2019-06-28
DK3092224T3 (en) 2018-11-26
AR099071A1 (es) 2016-06-29
US20180000807A1 (en) 2018-01-04
US20210121453A1 (en) 2021-04-29
US20190117638A1 (en) 2019-04-25
EP3092224B1 (en) 2018-08-22
PT3092224T (pt) 2018-11-14
RS57830B1 (sr) 2018-12-31
SMT201800619T1 (it) 2019-01-11
PL3092224T3 (pl) 2019-05-31
IL246599A0 (en) 2016-08-31
MX2016008898A (es) 2016-10-04
KR20160105885A (ko) 2016-09-07
TW201613884A (en) 2016-04-16
HRP20181585T1 (hr) 2018-12-14
UY35947A (es) 2015-07-31
JP6543259B2 (ja) 2019-07-10
JP2017502063A (ja) 2017-01-19
LT3092224T (lt) 2018-10-25
SG11201605618WA (en) 2016-08-30
US20200163949A1 (en) 2020-05-28
WO2015105772A1 (en) 2015-07-16
EA201691413A1 (ru) 2016-10-31
ES2693250T3 (es) 2018-12-10
US20190314358A1 (en) 2019-10-17
AU2015205001A1 (en) 2016-08-18
CA2936293A1 (en) 2015-07-16
US20180110766A1 (en) 2018-04-26
US20170258777A1 (en) 2017-09-14
US20150191452A1 (en) 2015-07-09
CN106061961A (zh) 2016-10-26
US20160081995A1 (en) 2016-03-24
EP3092224A1 (en) 2016-11-16
TR201815579T4 (tr) 2018-11-21
TWI640515B (zh) 2018-11-11
US9221796B2 (en) 2015-12-29
CL2016001763A1 (es) 2017-02-10
KR102311518B1 (ko) 2021-10-08
SI3092224T1 (sl) 2018-11-30
US20180250283A1 (en) 2018-09-06

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