BR112019001923A2 - moduladores de nmda de espiro-lactama e métodos de sua utilização - Google Patents

moduladores de nmda de espiro-lactama e métodos de sua utilização

Info

Publication number
BR112019001923A2
BR112019001923A2 BR112019001923-5A BR112019001923A BR112019001923A2 BR 112019001923 A2 BR112019001923 A2 BR 112019001923A2 BR 112019001923 A BR112019001923 A BR 112019001923A BR 112019001923 A2 BR112019001923 A2 BR 112019001923A2
Authority
BR
Brazil
Prior art keywords
spiro
methods
compounds
nmda modulators
lactam nmda
Prior art date
Application number
BR112019001923-5A
Other languages
English (en)
Inventor
Amin Khan M.
Original Assignee
Aptinyx Inc.
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 Aptinyx Inc. filed Critical Aptinyx Inc.
Publication of BR112019001923A2 publication Critical patent/BR112019001923A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C07D207/277Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D207/282-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pyrrole Compounds (AREA)

Abstract

são revelados compostos que possuem potência na modulação da atividade do receptor nmda. esses compostos podem ser usados no tratamento de condições como, por exemplo, depressão e distúrbios relacionados. formulações liberadas oralmente e outras formas de liberação farmaceuticamente aceitáveis dos compostos, incluindo formulações intravenosas, também são reveladas.
BR112019001923-5A 2016-08-01 2017-08-01 moduladores de nmda de espiro-lactama e métodos de sua utilização BR112019001923A2 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662369529P 2016-08-01 2016-08-01
US62/369,529 2016-08-01
US201762443915P 2017-01-09 2017-01-09
US62/443,915 2017-01-09
PCT/US2017/044871 WO2018026798A1 (en) 2016-08-01 2017-08-01 Spiro-lactam nmda modulators and methods of using same

Publications (1)

Publication Number Publication Date
BR112019001923A2 true BR112019001923A2 (pt) 2019-05-14

Family

ID=59593196

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112019001923-5A BR112019001923A2 (pt) 2016-08-01 2017-08-01 moduladores de nmda de espiro-lactama e métodos de sua utilização

Country Status (16)

Country Link
US (6) US11370790B2 (pt)
EP (1) EP3490990B1 (pt)
JP (2) JP2019527232A (pt)
KR (1) KR102538803B1 (pt)
CN (1) CN109843889B (pt)
AU (1) AU2017306164B2 (pt)
BR (1) BR112019001923A2 (pt)
CA (1) CA3031563C (pt)
CL (1) CL2019000245A1 (pt)
CO (1) CO2019000938A2 (pt)
IL (1) IL264482B (pt)
MX (1) MX2019001308A (pt)
PE (1) PE20190501A1 (pt)
PH (1) PH12019500208A1 (pt)
SG (1) SG11201900554YA (pt)
WO (1) WO2018026798A1 (pt)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5702288B2 (ja) 2008-09-18 2015-04-15 ノースウエスタン ユニバーシティ Nmdaレセプターモジュレータ及びその用途
LT3514158T (lt) 2013-01-29 2023-02-10 Aptinyx Inc. Spirolaktaminiai nmda receptoriaus moduliatoriai ir jų panaudojimas
MX2019001319A (es) 2016-08-01 2019-07-04 Aptinyx Inc Moduladores del receptor nmda espiro-lactam y uso de los mismos.
IL264482B (en) 2016-08-01 2022-09-01 Aptinyx Inc Spiro-lactam nmda modulators and methods of their use
BR112019001921A2 (pt) 2016-08-01 2019-05-14 Aptinyx Inc. moduladores do receptor nmda de espiro-lactama e seus usos
IL286107B1 (en) 2016-08-01 2024-05-01 Aptinyx Inc Spiro-lactam NMDA receptor modulators and their uses
EP3490994B8 (en) 2016-08-01 2024-03-13 Tenacia Biotechnology (Hong Kong) Co., Limited Spiro-lactam and bis-spiro-lactam nmda receptor modulators and uses thereof
WO2019152685A1 (en) * 2018-01-31 2019-08-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and methods of using same
KR20200115611A (ko) 2018-01-31 2020-10-07 앱티닉스 인크. 스피로-락탐 nmda 수용체 조정제 및 그의 용도
WO2019152696A1 (en) * 2018-01-31 2019-08-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
AU2020323543A1 (en) * 2019-08-01 2022-02-24 Aptinyx Inc. Methods of treating disorders associated with elevated levels of antibodies that interact with the NMDA receptor
US12012413B2 (en) 2019-11-11 2024-06-18 Tenacia Biotechnology (Hong Kong) Co., Limited Methods of treating painful diabetic peripheral neuropathy
WO2021112987A1 (en) * 2019-12-04 2021-06-10 Aptinyx Inc. Methods of treating cognitive impairment associated with neurodegenerative disease

Family Cites Families (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0180398A1 (en) 1984-10-26 1986-05-07 The Regents Of The University Of California Synthesis of beta-lactam
CA1305177C (en) 1987-06-30 1992-07-14 Yasufumi Ohfune Carboxycyclopropylglycine and process for producing the same
US4904681A (en) 1987-12-01 1990-02-27 G. D. Searle & Co. D-cycloserine and its prodrugs as cognitive enhancers
EP0360390A1 (en) 1988-07-25 1990-03-28 Glaxo Group Limited Spirolactam derivatives
US5061721A (en) 1989-03-15 1991-10-29 G. D. Searle & Co. Composition containing d-cycloserine and d-alanine for memory and learning enhancement or treatment of a cognitive or psychotic disorder
US5086072A (en) 1990-06-18 1992-02-04 The United States Of America As Represented By The Department Of Health And Human Services Treatment of mood disorders with functional antagonists of the glycine/nmda receptor complex
CA2058975C (en) 1990-10-30 2000-06-06 Shuichi Kasai Antiinflammatory gel preparation
US5168103A (en) 1991-01-22 1992-12-01 American Home Products Corporation [[2-(amino-3,4-dioxo-1-cyclobuten-1-yl) amino]alkyl]-acid derivatives
FR2692268B1 (fr) 1992-06-15 1994-08-19 Rhone Poulenc Rorer Sa Nouveaux polypeptides ayant une activité de récepteur NMDA, acides nucléiques codant pour ces polypeptides et utilisations.
SE9301667D0 (sv) 1993-05-14 1993-05-14 Kabi Pharmacia Ab New use
US5523323A (en) 1993-09-14 1996-06-04 Maccecchini; Maria-Luisa Use of partial agonists of the NMDA receptor to reduce opiate induced tolerance and dependence
US5605911A (en) 1995-01-31 1997-02-25 Washington University Use of alpha-2 adrenergic drugs to prevent adverse effects of NMDA receptor hypofunction (NRH)
US6335358B1 (en) 1995-04-12 2002-01-01 President And Fellows Of Harvard College Lactacystin analogs
US5741778A (en) 1996-03-19 1998-04-21 Amgen Inc. Method for treating Huntington's disease using glial cell line-derived neurotrophic factor (GDNF) protein product
US5763393A (en) 1996-05-17 1998-06-09 Neurotherapeutics L.P. Neuroactive peptides
PL330348A1 (en) 1996-06-07 1999-05-10 Zeneca Ltd Peptidic derivatives
JP2000503860A (ja) 1996-08-02 2000-04-04 ザイモジェネティクス,インコーポレイティド 精巣―特異的インシュリン同族体ポリペプチド
US5902815A (en) 1996-09-03 1999-05-11 Washington University Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction
JP3955345B2 (ja) 1996-09-27 2007-08-08 サントリー株式会社 新規アミノ酸ダイジハーベイン
AU1585999A (en) 1997-11-12 1999-05-31 Neurotherapeutics Methods for the detection and treatment of disease using a glycosyltransferase
US5952389A (en) 1998-01-13 1999-09-14 Synchroneuron Methods of treating tardive dyskinesia and other movement disorders
US6007841A (en) 1998-03-13 1999-12-28 Algos Pharmaceutical Corporation Analgesic composition and method for treating pain
US6274314B1 (en) 1998-04-02 2001-08-14 Nyxis Neurotherapies, Inc. Diagnostic assay for the modified nucleosides pseudouridine, 7-methyladenosine, or 1-methyladenosine
US6197820B1 (en) 1998-04-06 2001-03-06 Uab Research Foundation Use of phenylglycine derivatives to decrease neuronal death caused by brain tumors and brain lesions
US6025471A (en) 1998-06-03 2000-02-15 Deghenghi; Romano Diazaspiro, azepino and azabicyclo therapeutic peptides
WO2000027790A1 (en) 1998-11-11 2000-05-18 Smithkline Beecham P.L.C. Mutilin compounds
AU1724000A (en) 1998-11-12 2000-05-29 Nyxis, Inc. Diagnostic assay for cancer
US20030064921A1 (en) 1999-10-27 2003-04-03 The Regents Of The University Of California Methods and compounds for modulating melanocortin receptor ligand binding and activity
AU1922301A (en) 1999-11-17 2001-05-30 Nyxis Neurotherapies, Inc. Differential gene expression in cancer
WO2001057240A2 (en) 2000-02-01 2001-08-09 Agy Therapeutics, Inc. Interaction of nmda receptor with protein tyrosine phosphatase
JP2001261679A (ja) 2000-03-21 2001-09-26 Mitsui Chemicals Inc ピロリジノン誘導体及びそれらの製造方法並びに該化合物を含有する医薬
AU2001268467A1 (en) 2000-06-14 2001-12-24 Nyxis Neurotherapies, Inc. Identification of genes and compounds for treatment of cancer
EP1296999A2 (en) 2000-06-22 2003-04-02 NYXIS NeuroTherapies, Inc. Neuroactive peptides for treatment of hypoxia and related conditions
GB0018272D0 (en) 2000-07-25 2000-09-13 Vernalis Research Limited Chemical compounds IV
IL145209A0 (en) 2000-09-06 2002-06-30 Pfizer Prod Inc Pharmaceutical combinations for the treatment of stroke and traumatic brain injury
EP1186303A3 (en) 2000-09-06 2003-12-10 Pfizer Products Inc. Pharmaceutical combinations, for the treatment of stroke and traumatic brain injury, containing a neutrophil inhibiting factor and an selective NMDA-NR2B receptor antagonist
UA73619C2 (en) 2000-12-13 2005-08-15 Pfizer Prod Inc Stable pharmaceutical compositions of nmda receptor agonist (variants) and method of treatment
US20020142287A1 (en) 2000-12-14 2002-10-03 Hirotaka Yamamoto High throughput assay to detect inhibitors of the map kinase pathway
WO2002072005A2 (en) 2001-03-07 2002-09-19 University Of Utah Research Foundation Linear y-carboxyglutamate rich conotoxins
WO2002072609A2 (en) 2001-03-12 2002-09-19 Nyxis Neurotherapies, Inc Neuroactive peptides for prevention and/or treatment of hypoxia and neuropathic pain
US20030022253A1 (en) 2001-07-25 2003-01-30 Nyxis Neurotherapies, Inc. Method for identifying, isolating and producing neuroactive binding agents and binding agents derived thereby
WO2004005293A2 (en) 2002-07-05 2004-01-15 Targacept, Inc. N-aryl diazaspiracyclic compounds and methods of preparation and use thereof
US7273889B2 (en) 2002-09-25 2007-09-25 Innovative Drug Delivery Systems, Inc. NMDA receptor antagonist formulation with reduced neurotoxicity
AU2004232939A1 (en) 2003-04-17 2004-11-04 Merck Sharp & Dohme Corp. Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
WO2005007656A1 (en) 2003-07-18 2005-01-27 Virochem Pharma Inc. Spiro compounds and methods for the modulation of chemokine receptor activity
CA2534909A1 (en) 2003-08-08 2005-02-17 The Burnham Institute P16 mediated regulation of nmda receptors
WO2005020973A2 (en) 2003-08-29 2005-03-10 The University Of Houston System Compositions having antimycrobial activity including a hydroxamate or a hydroxamate and a hydroxylamine
GB0323204D0 (en) 2003-10-03 2003-11-05 Novartis Ag Organic compounds
US20050096311A1 (en) 2003-10-30 2005-05-05 Cns Response Compositions and methods for treatment of nervous system disorders
WO2005047286A1 (ja) 2003-11-13 2005-05-26 Ono Pharmaceutical Co., Ltd. スピロ複素環化合物
BRPI0418375A (pt) 2004-01-08 2007-05-22 Hoffmann La Roche derivados de diaza-espiropiperidina
US20060063707A1 (en) 2004-09-17 2006-03-23 Lifelike Biomatic, Inc. Compositions for enhancing memory and methods therefor
CN101090902B (zh) 2004-10-13 2013-05-29 默沙东公司 Cgrp受体拮抗剂
EP2030622B1 (en) 2005-03-24 2011-02-23 Emory University Indication of dosage of progesterone in the treatment of a traumatic brain injury
JP5261178B2 (ja) 2005-08-26 2013-08-14 ウィスコンシン アルムニ リサーチ ファンデイション 官能化されたベータラクタムモノマーからのポリ−ベータ−ペプチド及びポリ−ベータ−ペプチドを含有する抗菌組成物
AR059224A1 (es) 2006-01-31 2008-03-19 Jerini Ag Compuestos para la inhibicion de integrinas y uso de estas
US20070208001A1 (en) 2006-03-03 2007-09-06 Jincong Zhuo Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
MX2009002921A (es) 2006-09-15 2009-04-01 Schering Corp Derivados de azetidinona para el tratamiento de trastornos del metabolismo lipidico.
JP2008188285A (ja) 2007-02-06 2008-08-21 Bridgestone Corp バックパッド及び車両用シート
CA2682195A1 (en) 2007-03-20 2008-09-25 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CN101066945B (zh) 2007-05-25 2010-05-19 中国科学院上海有机化学研究所 一种合成3-位取代内酰胺类化合物的方法
CN101125817B (zh) 2007-08-03 2011-09-14 中国科学院上海有机化学研究所 一种合成高对映选择性醛基取代小环胺类化合物和光学活性3-位取代内酰胺类化合物的方法
US20090054392A1 (en) 2007-08-20 2009-02-26 Wyeth Naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system
WO2009039390A2 (en) 2007-09-20 2009-03-26 Naurex Inc. The development of glycobiology-based therapeutics for the treatment of brain tumors
WO2009105718A1 (en) 2008-02-20 2009-08-27 The Children's Hospital Of Philadelphia Genetic alterations associated with autism and the autistic phenotype and methods of use thereof for the diagnosis and treatmemt of autism
US20110105480A1 (en) * 2008-06-24 2011-05-05 Keith Freehauf Pharmaceutical transdermal compositions and method for treating inflammation in cattle
CN102076679A (zh) 2008-06-27 2011-05-25 神经研究公司 新颖的四甲基取代的哌啶衍生物及其作为单胺神经递质再摄取抑制剂的用途
KR101647520B1 (ko) 2008-08-07 2016-08-10 에프. 호프만-라 로슈 아게 거대환식 화합물의 제조 방법
GB0814991D0 (en) 2008-08-15 2008-09-24 Glaxo Group Ltd Compounds
JP5702288B2 (ja) 2008-09-18 2015-04-15 ノースウエスタン ユニバーシティ Nmdaレセプターモジュレータ及びその用途
WO2010065709A2 (en) 2008-12-03 2010-06-10 Amin Khan Hydroxamic acid derivatives, preparation and therapeutic uses thereof
DE102009001460B4 (de) 2009-03-11 2010-12-02 Zf Friedrichshafen Ag Ölbehälter
US8329904B2 (en) 2009-05-12 2012-12-11 Hoffmann-La Roche Inc. Azacyclic derivatives
US20120178695A1 (en) 2009-07-02 2012-07-12 Joseph Moskal Methods of treating neuropathic pain
EP3488856A1 (en) 2009-10-05 2019-05-29 Northwestern University Methods of treating depression and other related diseases
US8951968B2 (en) 2009-10-05 2015-02-10 Northwestern University Methods of treating depression and other related diseases
US8871208B2 (en) 2009-12-04 2014-10-28 Abbvie Inc. 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors and uses thereof
JP2013515033A (ja) 2009-12-21 2013-05-02 ノバルティス アーゲー オレキシン受容体アンタゴニストとしてのジアザ−スピロ[5.5]ウンデカン類
BR112012020142A2 (pt) 2010-02-11 2020-08-18 Northwestern University moduladores do receptor de nmda com estrutura secundária estabilizada e usos dos mesmos.
KR101692275B1 (ko) 2010-02-11 2017-01-04 노오쓰웨스턴 유니버시티 2차 구조 안정화된 nmda 수용체 조절제 및 그의 용도
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
US8097634B2 (en) 2010-04-15 2012-01-17 Hoffmann-La Roche Inc. Azacyclic derivatives
GB201007789D0 (en) 2010-05-10 2010-06-23 Glaxo Group Ltd Novel Compound
CN102267995A (zh) 2010-06-04 2011-12-07 艾琪康医药科技(上海)有限公司 一种制备二氮杂螺环化合物的方法
WO2012021712A1 (en) 2010-08-12 2012-02-16 Tetraphase Pharmaceuticals, Inc. Tetracycline analogs
US9737531B2 (en) 2012-07-12 2017-08-22 Glytech, Llc Composition and method for treatment of depression and psychosis in humans
EP2678338B1 (en) * 2011-02-25 2015-09-09 Novartis AG Pyrazolo[1,5-a]pyridines as trk inhibitors
AU2012229172B2 (en) 2011-03-14 2017-02-09 Alkahest, Inc. Benzodioxane inhibitors of leukotriene production
SG10202010665YA (en) 2011-04-27 2020-11-27 Univ Northwestern Methods of treating alzheimer's disease, huntington's disease, autism, or other disorders
US9293690B2 (en) 2011-06-27 2016-03-22 Koninklijke Philips N.V. Ultrasound transducer assembly and method of manufacturing the same
WO2013010275A1 (en) * 2011-07-18 2013-01-24 The Governors Of The University Of Alberta Catalysts and processes for the hydrogenation of amides
DK3333161T3 (da) 2011-07-27 2020-05-18 Astrazeneca Ab 2-(2,4,5-substitueret anilin)-pyrimidinderivater som egfr-modulatorer, der er anvendelige til behandling af cancer
US9546179B2 (en) * 2011-12-20 2017-01-17 Wei Qian Heterocycle amido alkyloxy substituted quinazoline derivative and use thereof
AR092031A1 (es) 2012-07-26 2015-03-18 Merck Sharp & Dohme Inhibidores del canal de potasio medular externo renal
CN102936216B (zh) * 2012-12-05 2015-03-04 南京药石药物研发有限公司 7,9-二氧代-2,6-氮杂-螺[3.5]壬-2-甲酸叔丁酯及其中间体的制备方法
WO2014120784A1 (en) 2013-01-29 2014-08-07 Naurex, Inc. Spiro-lactam nmda receptor modulators and uses thereof
CA2899191A1 (en) 2013-01-29 2014-08-07 Naurex, Inc. Spiro-lactam nmda receptor modulators and uses thereof
SG11201505934XA (en) 2013-01-29 2015-09-29 Naurex Inc Spiro-lactam nmda receptor modulators and uses thereof
LT3514158T (lt) 2013-01-29 2023-02-10 Aptinyx Inc. Spirolaktaminiai nmda receptoriaus moduliatoriai ir jų panaudojimas
WO2014120789A1 (en) * 2013-01-29 2014-08-07 Naurex, Inc. Spiro-lactam nmda receptor modulators and uses thereof
CN103171641B (zh) 2013-03-19 2015-07-15 浙江大学 具备轮动功能的弹跳机器人
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
GB2528480A (en) * 2014-07-23 2016-01-27 Givaudan Sa Improvements in or relating to organic compounds
GB201416346D0 (en) 2014-09-16 2014-10-29 Shire Internat Gmbh Spirocyclic derivatives
PE20190174A1 (es) 2016-05-19 2019-02-01 Aptinyx Inc Moduladores del receptor espiro-lactama n-metil-d-aspartato y usos de los mismos
WO2017201285A1 (en) 2016-05-19 2017-11-23 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
IL264482B (en) 2016-08-01 2022-09-01 Aptinyx Inc Spiro-lactam nmda modulators and methods of their use
EP3490994B8 (en) 2016-08-01 2024-03-13 Tenacia Biotechnology (Hong Kong) Co., Limited Spiro-lactam and bis-spiro-lactam nmda receptor modulators and uses thereof
MX2019001319A (es) 2016-08-01 2019-07-04 Aptinyx Inc Moduladores del receptor nmda espiro-lactam y uso de los mismos.
BR112019001921A2 (pt) 2016-08-01 2019-05-14 Aptinyx Inc. moduladores do receptor nmda de espiro-lactama e seus usos
IL286107B1 (en) 2016-08-01 2024-05-01 Aptinyx Inc Spiro-lactam NMDA receptor modulators and their uses
KR20200115611A (ko) 2018-01-31 2020-10-07 앱티닉스 인크. 스피로-락탐 nmda 수용체 조정제 및 그의 용도
PE20211455A1 (es) 2018-01-31 2021-08-05 Aptinyx Inc Moduladores del receptor nmda espiro-lactama y usos de los mismos
US12012413B2 (en) 2019-11-11 2024-06-18 Tenacia Biotechnology (Hong Kong) Co., Limited Methods of treating painful diabetic peripheral neuropathy
US20210308101A1 (en) 2019-11-11 2021-10-07 Aptinyx Inc. Methods of treating fibromyalgia
WO2021112987A1 (en) 2019-12-04 2021-06-10 Aptinyx Inc. Methods of treating cognitive impairment associated with neurodegenerative disease

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